[CAS NO. 1373431-65-2] Talazoparib tosylate

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PRODUCTS SPECIFICATIONS [1373431-65-2]

Catalog

HY-108413

Brand

MCE

CAS

1373431-65-2

DESCRIPTION [1373431-65-2]

Overview

MDL	-
Molecular Weight	552.55
Molecular Formula	C26H22F2N6O4S
SMILES	O=C1NN=C2C3=C1C=C(F)C=C3N[C@H](C4=CC=C(F)C=C4)[C@H]2C5=NC=NN5C.O=S(C6=CC=C(C)C=C6)(O)=O

For research use only. We do not sell to patients.

45 Publications Citing Use of MCE

Summary

Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC ₅₀ of 0.57 nM for PARP1 .

IC50 & Target

IC50: 0.57 nM (PARP1) ^[1]

In Vitro

Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC ₅₀ =0.57 nM), it has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant (K _D ) of 0.29 nM. Talazoparib inhibits PARP1 and -2 to a similar extent, with K _i s of 1.20 and 0.85 nM, respectively. Talazoparib selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib targets tumor cells with homologous recombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice. Synergistic or additive antitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05059522	Pfizer	Advanced Malignancies\|NSCLC\|Ovarian Cancer\|Urothelial Cancer\|Solid Tumors	September 29, 2021	Phase 3
NCT04690855	Mylin A. Torres, MD\|Genentech, Inc.\|Pfizer\|Emory University\|Hoosier Cancer Research Network	Breast Cancer\|Triple Negative Breast Cancer	April 1, 2021	Phase 2
NCT02127151	University College, London\|Medivation, Inc.	Endometrial Cancer	October 1, 2014	Phase 2
NCT03377556	Southwest Oncology Group\|National Cancer Institute (NCI)	ATM Gene Mutation\|ATR Gene Mutation\|BARD1 Gene Mutation\|BRCA1 Gene Mutation\|BRCA2 Gene Mutation\|BRIP1 Gene Mutation\|CHEK1 Gene Mutation\|CHEK2 Gene Mutation\|FANCA Gene Mutation\|FANCC Gene Mutation\|FANCD2 Gene Mutation\|FANCF Gene Mutation\|FANCM Gene Mutation\|NBN Gene Mutation\|PALB2 Gene Mutation\|RAD51 Gene Mutation\|RAD51B Gene Mutation\|RAD54L Gene Mutation\|Recurrent Squamous Cell Lung Carcinoma\|RPA1 Gene Mutation\|Stage IV Squamous Cell Lung Carcinoma AJCC v7	March 3, 2017	Phase 2
NCT02049593	Jonsson Comprehensive Cancer Center\|Translational Research in Oncology\|BioMarin Pharmaceutical\|Medivation, Inc.	Metastatic Cancer\|Unspecified Adult Solid Tumor	June 12, 2014	Phase 1
NCT02154490	Southwest Oncology Group\|National Cancer Institute (NCI)	Recurrent Squamous Cell Lung Carcinoma\|Stage IV Squamous Cell Lung Carcinoma AJCC v7	June 16, 2014
NCT04187833	Case Comprehensive Cancer Center	Metastatic or Unresectable Melanoma	June 5, 2020	Phase 2
NCT02627430	National Cancer Institute (NCI)	Adult Solid Neoplasm\|Estrogen Receptor Negative\|Fallopian Tube Serous Neoplasm\|HER2+Neu Negative\|Ovarian Serous Adenocarcinoma\|Ovarian Serous Tumor\|Primary Peritoneal Serous Adenocarcinoma\|Progesterone Receptor Negative\|Recurrent Breast Carcinoma\|Recurrent Fallopian Tube Carcinoma\|Recurrent Ovarian Carcinoma\|Recurrent Primary Peritoneal Carcinoma\|Triple-Negative Breast Carcinoma	March 2016	Phase 1
NCT02358200	Pamela Munster\|QuantumLeap Healthcare Collaborative\|University of California, San Francisco	Triple Negative Metastatic Breast Cancer\|BRCA-mutated Solid Tumor	February 23, 2015	Phase 1
NCT04039230	Massachusetts General Hospital\|Pfizer	Breast Cancer	October 9, 2019	Phase 1\|Phase 2
NCT05071937	Haider Mahdi\|Pfizer\|Zenith Epigenetics\|University of Pittsburgh	Ovarian Cancer\|Peritoneal Cancer\|Fallopian Tube Cancer	April 27, 2022	Phase 2
NCT01776437	Pfizer	Human Volunteers	February 2013	Phase 1
NCT04987931	Pfizer	Breast Cancer	August 20, 2021
NCT03964532	Georgetown University\|Pfizer	Breast Cancer	April 17, 2019	Phase 1\|Phase 2
NCT04846478	Dana-Farber Cancer Institute\|Epizyme, Inc.\|Pfizer	Metastatic Prostate Cancer\|Metastatic Castration-resistant Prostate Cancer	June 28, 2021	Phase 1
NCT03565991	Pfizer	Locally Advanced or Metastatic Solid Tumors\|Genes, BRCA 1	June 18, 2018	Phase 2
NCT05053854	Peter MacCallum Cancer Centre, Australia	Neuroendocrine Tumors	December 8, 2021	Phase 1
NCT03395197	Pfizer\|Astellas Pharma Inc	mCRPC	December 18, 2017	Phase 3
NCT04734730	City of Hope Medical Center\|National Cancer Institute (NCI)	Castration-Sensitive Prostate Carcinoma\|Metastatic Prostate Adenocarcinoma\|Stage IV Prostate Cancer AJCC v8\|Stage IVA Prostate Cancer AJCC v8\|Stage IVB Prostate Cancer AJCC v8	May 4, 2021	Phase 2
NCT02912572	Dana-Farber Cancer Institute\|Pfizer	Metastatic Endometrial Cancer	November 14, 2016	Phase 2
NCT04337970	Memorial Sloan Kettering Cancer Center	Kidney Cancer\|Renal Cell Carcinoma\|Unresectable Renal Cell Carcinoma\|Metastatic Renal Cell Carcinoma	April 6, 2020	Phase 1\|Phase 2
NCT03875313	Calithera Biosciences, Inc	Solid Tumor\|Clear Cell Renal Cell Carcinoma\|TNBC - Triple-Negative Breast Cancer\|Colorectal Cancer\|CRC\|RCC\|ccRCC	May 20, 2019	Phase 1\|Phase 2
NCT04693468	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|Metastatic Malignant Solid Neoplasm\|Recurrent Malignant Solid Neoplasm	December 1, 2020	Phase 1
NCT03968406	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Malignant Female Reproductive System Neoplasm\|Recurrent Cervical Carcinoma\|Recurrent Endometrial Carcinoma\|Recurrent Fallopian Tube Carcinoma\|Recurrent Ovarian Carcinoma\|Recurrent Primary Peritoneal Carcinoma\|Recurrent Vaginal Carcinoma\|Stage IV Cervical Cancer AJCC v8\|Stage IV Fallopian Tube Cancer AJCC v8\|Stage IV Ovarian Cancer AJCC v8\|Stage IV Primary Peritoneal Cancer AJCC v8\|Stage IV Uterine Corpus Cancer AJCC v8\|Stage IV Vaginal Cancer AJCC v8\|Stage IVA Cervical Cancer AJCC v8\|Stage IVA Fallopian Tube Cancer AJCC v8\|Stage IVA Ovarian Cancer AJCC v8\|Stage IVA Primary Peritoneal Cancer AJCC v8\|Stage IVA Uterine Corpus Cancer AJCC v8\|Stage IVA Vaginal Cancer AJCC v8\|Stage IVB Cervical Cancer AJCC v8\|Stage IVB Fallopian Tube Cancer AJCC v8\|Stage IVB Ovarian Cancer AJCC v8\|Stage IVB Primary Peritoneal Cancer AJCC v8\|Stage IVB Uterine Corpus Cancer AJCC v8\|Stage IVB Vaginal Cancer AJCC v8	September 26, 2019	Phase 1
NCT02317874	National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|Metastatic Malignant Solid Neoplasm\|Unresectable Malignant Solid Neoplasm	July 24, 2015	Phase 1
NCT03974217	Dana-Farber Cancer Institute\|Pfizer	Leukemia	August 1, 2019	Phase 1
NCT03499353	Pfizer	Early Breast Cancer	August 27, 2018	Phase 2
NCT04462809	Hospices Civils de Lyon	Advanced Malignant Pleural or Peritoneal Mesothelioma	September 1, 2020	Phase 2
NCT05035745	National University Hospital, Singapore	Advanced Refractory Solid Tumors\|Advanced Triple Negative Breast Cancers\|Metastatic Triple Negative Breast Cancers	March 1, 2021	Phase 1\|Phase 2
NCT03343054	Pfizer	Neoplasms\|Breast Neoplasms	November 30, 2017	Phase 1
NCT04052204	Pfizer\|EMD Serono\|Nektar Therapeutics\|Astellas Pharma Inc	Squamous Cell Carcinoma of the Head and Neck (SCCHN)\|Metastatic Castration Resistant Prostate Cancer (mCRPC)	December 30, 2019	Phase 1\|Phase 2
NCT02693535	American Society of Clinical Oncology\|AstraZeneca\|Bayer\|Bristol-Myers Squibb\|Eli Lilly and Company\|Genentech, Inc.\|Merck Sharp & Dohme LLC\|Pfizer\|Boehringer Ingelheim\|Seagen Inc.	Lymphoma, Non-Hodgkin\|Multiple Myeloma\|Advanced Solid Tumors	March 14, 2016	Phase 2
NCT04901702	St. Jude Children´s Research Hospital\|Pfizer\|Ipsen	Recurrent Solid Tumor\|Recurrent Ewing Sarcoma\|Recurrent Hepatoblastoma\|Recurrent Malignant Germ Cell Tumor\|Recurrent Malignant Solid Neoplasm\|Recurrent Neuroblastoma\|Recurrent Osteosarcoma\|Recurrent Peripheral Primitive Neuroectodermal Tumor\|Recurrent Rhabdoid Tumor\|Recurrent Rhabdomyosarcoma\|Recurrent Soft Tissue Sarcoma\|Recurrent Wilms Tumor\|Refractory Ewing Sarcoma\|Refractory Hepatoblastoma\|Refractory Malignant Germ Cell Tumor\|Refractory Malignant Solid Neoplasm\|Refractory Neuroblastoma\|Refractory Osteosarcoma\|Refractory Peripheral Primitive Neuroectodermal Tumor\|Refractory Rhabdoid Tumor\|Refractory Rhabdomyosarcoma\|Refractory Soft Tissue Sarcoma	June 9, 2021	Phase 1\|Phase 2
NCT04511039	Roswell Park Cancer Institute\|Pfizer	Advanced Malignant Solid Neoplasm\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma\|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma\|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma A\|Locally Advanced Colorectal Carcinoma\|Locally Advanced Gastroesophageal Junction Adenocarcinoma\|Metastatic Colorectal Adenocarcinoma\|Metastatic Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma\|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma\|Postneoadjuvant Therapy Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Postneoadjuvant Therapy Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Stage III Colorectal Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	May 28, 2021	Phase 1
NCT02878785	University of Maryland, Baltimore\|Pfizer\|Van Andel Research Institute	Acute Myeloid Leukemia	August 2016	Phase 1\|Phase 2
NCT05319249	German Cancer Research Center	Acute Myeloid Leukemia	September 2022	Phase 1\|Phase 2
NCT04019327	Memorial Sloan Kettering Cancer Center	Prostate Cancer\|Prostate Adenocarcinoma\|Prostate Neoplasm\|Prostate Cancer Metastatic\|Castration-resistant Prostate Cancer	July 11, 2019	Phase 1\|Phase 2
NCT04678362	Centre Francois Baclesse\|Pfizer	Urothelial Carcinoma	June 1, 2021	Phase 2
NCT04334941	National Cancer Institute (NCI)	Extensive Stage Lung Small Cell Carcinoma	June 15, 2020	Phase 2
NCT01989546	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Advanced Ovarian Cancer\|Primary Peritoneal Cancer\|Advanced Breast Cancer\|Advanced Solid Tumors	February 4, 2014	Phase 1\|Phase 2
NCT05327010	National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|Advanced Ovarian Carcinoma\|Metastatic Malignant Solid Neoplasm\|Metastatic Ovarian Carcinoma\|Recurrent Malignant Solid Neoplasm\|Refractory Malignant Solid Neoplasm\|Stage III Ovarian Cancer AJCC v8\|Stage IV Ovarian Cancer AJCC v8	August 4, 2022	Phase 2
NCT01399840	Pfizer\|Medivation, Inc.	Acute Myeloid Leukemia\|Myelodysplastic Syndrome\|Chronic Lymphocytic Leukemia\|Mantle Cell Lymphoma	June 30, 2011	Phase 1
NCT04635631	Pfizer	Neoplasms	November 30, 2020	Phase 1
NCT02921919	Pfizer\|Medivation, Inc.	Cancer	November 8, 2016	Phase 2
NCT04486352	Alliance Foundation Trials, LLC.\|Genentech, Inc.\|Foundation Medicine\|Pfizer	Endometrial Cancer	October 20, 2021	Phase 1\|Phase 2
NCT02997163	Pfizer\|Medivation, Inc.	Advanced Solid Tumors	February 21, 2017	Phase 1
NCT02282345	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Breast Adenocarcinoma\|Deleterious BRCA1 Gene Mutation\|Deleterious BRCA2 Gene Mutation\|HER2+Neu Negative\|Invasive Breast Carcinoma	April 16, 2015	Phase 2
NCT02925234	The Netherlands Cancer Institute\|Amgen\|AstraZeneca\|Bayer\|Bristol-Myers Squibb\|Novartis\|Roche Pharma AG\|Merck Sharp & Dohme LLC\|Boehringer Ingelheim\|Ipsen\|Eisai Inc.\|Pfizer\|Clovis Oncology, Inc.\|Eli Lilly and Company\|Janssen, LP	Cancer\|Tumors\|Neoplasm\|Neoplasia	August 2016	Phase 2
NCT03042910	Pfizer\|Medivation, Inc.	Solid Tumor	October 13, 2016	Phase 1
NCT02034916	Pfizer\|Myriad Genetic Laboratories, Inc.\|Medivation, Inc.	Breast Neoplasms\|BRCA 1 Gene Mutation\|BRCA 2 Gene Mutation	December 13, 2013	Phase 2
NCT03426254	Center Trials & Treatment\|BioGene Pharmaceutical	Advanced or Recurrent Solid Tumors\|Breast Neoplasm	November 10, 2022	Phase 1
NCT04824937	Massachusetts General Hospital\|Calithera Biosciences, Inc\|Pfizer\|Prostate Cancer Foundation	Prostate Cancer Metastatic	July 2021	Phase 2
NCT03148795	Pfizer\|Medivation, Inc.	Prostate Cancer	July 4, 2017	Phase 2
NCT04821622	Pfizer\|Astellas Pharma Inc	Prostate Cancer	May 12, 2021	Phase 3
NCT03672773	Jonsson Comprehensive Cancer Center\|Translational Research in Oncology\|Pfizer	Recurrent Extensive Stage Small Cell Lung Carcinoma\|Refractory Extensive Stage Small Cell Lung Carcinoma	October 31, 2018	Phase 2
NCT04892693	Seoul National University Hospital	Advanced Breast Cancer	May 25, 2021	Phase 2
NCT04170946	University Health Network, Toronto\|Pfizer	Lung Cancer\|Small-Cell Lung Cancer	October 5, 2020	Phase 1
NCT03642132	Pfizer	Ovarian Cancer	July 19, 2018	Phase 3
NCT03637491	Pfizer	Pancreatic Cancer	August 15, 2018	Phase 1\|Phase 2
NCT04756765	Stanford University\|Pfizer	Breast Cancer\|Advanced Breast Cancer	January 2023	Phase 2
NCT04173507	Southwest Oncology Group\|National Cancer Institute (NCI)	Advanced Lung Non-Squamous Non-Small Cell Carcinoma\|Recurrent Lung Non-Squamous Non-Small Cell Carcinoma\|Stage IV Lung Cancer AJCC v8\|Stage IVA Lung Cancer AJCC v8\|Stage IVB Lung Cancer AJCC v8	February 14, 2020	Phase 2
NCT02116777	National Cancer Institute (NCI)	Adult Solid Neoplasm\|Childhood Solid Neoplasm\|Recurrent Childhood Central Nervous System Neoplasm\|Recurrent Ewing Sarcoma+Peripheral Primitive Neuroectodermal Tumor\|Recurrent Malignant Solid Neoplasm\|Refractory Central Nervous System Neoplasm	May 16, 2014	Phase 1\|Phase 2
NCT04134884	Kathy Miller\|Pfizer\|Astex Pharmaceuticals, Inc.\|Van Andel Institute Stand Up to Cancer Team\|Indiana University	Metastatic Breast Cancer\|Triple Negative Breast Cancer\|Hormone Receptor Positive Tumor	March 30, 2020	Phase 1
NCT04991480	Artios Pharma Ltd	Advanced Cancer\|Metastatic Cancer\|Breast Cancer	September 13, 2021	Phase 1\|Phase 2
NCT04849364	Bryan Schneider, MD\|Genentech, Inc.\|Pfizer\|Foundation Medicine\|Indiana University\|Epic Sciences\|Vera Bradley Foundation for Breast Cancer Research\|Hoosier Cancer Research Network	Breast Cancer\|Triple Negative Breast Cancer	August 24, 2021	Phase 2
NCT05142241	National Cancer Institute (NCI)	Adrenal Gland Pheochromocytoma\|Hematopoietic and Lymphoid System Neoplasm\|Malignant Solid Neoplasm\|Paraganglioma	March 23, 2022	Phase 2
NCT03911973	Kari Wisinski\|Pfizer\|Big Ten Cancer Research Consortium	TNBC - Triple-Negative Breast Cancer	April 17, 2019	Phase 1\|Phase 2
NCT03990896	Massachusetts General Hospital\|Pfizer	Breast Cancer	November 18, 2021	Phase 2
NCT05288127	University of Malaya\|Cancer Research Malaysia\|Pfizer\|Pantai Hospital Kuala Lumpur\|Hospital Sultan Ismail	HRD 100 Gene Expression High\|Triple Negative Breast Cancer	March 8, 2022	Phase 2
NCT02401347	Melinda Telli\|BioMarin Pharmaceutical\|Pfizer\|Stanford University	Advanced Breast Cancer\|HER2+Neu Negative\|Triple-Negative Breast Cancer	August 2015	Phase 2
NCT04497116	Repare Therapeutics\|Roche Pharma AG	Advanced Solid Tumor	July 22, 2020	Phase 1\|Phase 2
NCT04207190	Roswell Park Cancer Institute\|Pfizer	Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia	October 23, 2020	Phase 1\|Phase 2
NCT04332744	MedSIR\|Pfizer	Metastatic Prostate Cancer	September 2, 2020	Phase 2
NCT03077607	Pfizer\|Medivation, Inc.	Advanced Solid Tumors	November 7, 2016	Phase 1
NCT05141708	Pfizer	Metastatic Breast Cancer\|Breast Neoplasms	December 17, 2021
NCT02537561	Washington University School of Medicine\|BioMarin Pharmaceutical	Solid Tumors\|Carcinoma, Non-Small Cell Lung\|Non-Small Cell Lung Cancer\|Non-Small-Cell Lung Carcinoma\|Nonsmall Cell Lung Cancer	December 2015	Phase 1
NCT02567396	National Cancer Institute (NCI)	Estrogen Receptor Negative\|Head and Neck Squamous Cell Carcinoma\|HER2+Neu Negative\|Hormone-Resistant Prostate Cancer\|Metastatic Pancreatic Adenocarcinoma\|Progesterone Receptor Negative\|Solid Neoplasm\|Stage III Mesothelioma\|Stage IIIA Gastric Cancer\|Stage IIIA Non-Small Cell Lung Cancer\|Stage IIIA Ovarian Cancer\|Stage IIIA Small Cell Lung Carcinoma\|Stage IIIB Gastric Cancer\|Stage IIIB Non-Small Cell Lung Cancer\|Stage IIIB Ovarian Cancer\|Stage IIIB Small Cell Lung Carcinoma\|Stage IIIC Gastric Cancer\|Stage IIIC Ovarian Cancer\|Stage IV Mesothelioma\|Stage IV Non-Small Cell Lung Cancer\|Stage IV Ovarian Cancer\|Stage IV Small Cell Lung Carcinoma\|Triple-Negative Breast Carcinoma	June 2016	Phase 1
NCT03330405	Pfizer	Avelumab in Combination With Talazoparib Will be Investigated in Patients With Locally Advanced (Primary or Recurrent) or Metastatic Solid Tumors	October 19, 2017	Phase 2
NCT02836028	Pfizer\|Myriad Genetic Laboratories, Inc.\|Medivation, Inc.	Ovarian Cancer	October 2016	Phase 2
NCT01042379	QuantumLeap Healthcare Collaborative	Breast Neoplasms\|Breast Cancer\|Breast Tumors\|Angiosarcoma\|TNBC - Triple-Negative Breast Cancer\|HER2-positive Breast Cancer\|HER2-negative Breast Cancer\|Hormone Receptor Positive Tumor\|Hormone Receptor Negative Tumor\|Early-stage Breast Cancer\|Locally Advanced Breast Cancer	March 1, 2010	Phase 2
NCT05097599	Strata Oncology	Cancer\|Advanced Solid Tumor	November 19, 2021	Phase 2
NCT02316834	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Fallopian Tube Serous Adenocarcinoma\|High Grade Ovarian Serous Adenocarcinoma\|Ovarian Mass\|Primary Peritoneal Serous Adenocarcinoma\|Stage III Fallopian Tube Cancer AJCC v7\|Stage III Ovarian Cancer AJCC v6 and v7\|Stage III Primary Peritoneal Cancer AJCC v7\|Stage IIIA Fallopian Tube Cancer AJCC v7\|Stage IIIA Ovarian Cancer AJCC v6 and v7\|Stage IIIA Primary Peritoneal Cancer AJCC v7\|Stage IIIB Fallopian Tube Cancer AJCC v7\|Stage IIIB Ovarian Cancer AJCC v6 and v7\|Stage IIIB Primary Peritoneal Cancer AJCC v7\|Stage IIIC Fallopian Tube Cancer AJCC v7\|Stage IIIC Ovarian Cancer AJCC v6 and v7\|Stage IIIC Primary Peritoneal Cancer AJCC v7\|Stage IV Fallopian Tube Cancer AJCC v6 and v7\|Stage IV Ovarian Cancer AJCC v6 and v7\|Stage IV Primary Peritoneal Cancer AJCC v7	June 2, 2015	Early Phase 1
NCT03070548	Pfizer\|Medivation, Inc.	Advanced Solid Tumors	September 2016	Phase 1
NCT05101551	Stanford University	Acute Myeloid Leukemia	November 2022	Phase 1
NCT03901469	Zenith Epigenetics\|Pfizer\|Newsoara Biopharma Co., Ltd.	Triple Negative Breast Cancer	June 26, 2019	Phase 2
NCT02997176	Pfizer\|Medivation, Inc.	Advanced Solid Tumors	September 30, 2016	Phase 1
NCT01945775	Pfizer\|Medivation, Inc.	Breast Neoplasms\|BRCA 1 Gene Mutation\|BRCA 2 Gene Mutation	October 14, 2013	Phase 3
NCT01286987	Pfizer\|Medivation, Inc.	Advanced or Recurrent Solid Tumors\|Breast Neoplasms\|Ovarian Cancer, Epithelial\|Ewing Sarcoma\|Small Cell Lung Carcinoma\|Prostate Cancer\|Pancreas Cancer	January 3, 2011	Phase 1
NCT04068831	Memorial Sloan Kettering Cancer Center	Metastatic Renal Cell Carcinoma\|Fumarate Hydratase Deficient Renal Cell Carcinoma\|Succinate Dehydrogenase Deficient Renal Cell Carcinoma	August 22, 2019	Phase 2
NCT02326844	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Ovarian Cancer	March 2, 2015	Phase 2
NCT05425862	Peter MacCallum Cancer Centre, Australia	Metastatic Castration Resistant Prostate Cancer (mCRPC)	October 21, 2022	Phase 1
NCT04550494	National Cancer Institute (NCI)	Advanced Pancreatic Carcinoma\|Anatomic Stage III Breast Cancer AJCC v8\|Anatomic Stage IV Breast Cancer AJCC v8\|Castration-Resistant Prostate Carcinoma\|Clinical Stage III Gastric Cancer AJCC v8\|Clinical Stage IV Gastric Cancer AJCC v8\|HER2-Positive Breast Carcinoma\|Locally Advanced Breast Carcinoma\|Locally Advanced Gastric Carcinoma\|Locally Advanced Malignant Solid Neoplasm\|Locally Advanced Ovarian Carcinoma\|Locally Advanced Pancreatic Carcinoma\|Locally Advanced Prostate Carcinoma\|Metastatic Breast Carcinoma\|Metastatic Gastric Carcinoma\|Metastatic Malignant Solid Neoplasm\|Metastatic Ovarian Carcinoma\|Metastatic Pancreatic Carcinoma\|Metastatic Prostate Carcinoma\|Platinum-Sensitive Ovarian Carcinoma\|Postneoadjuvant Therapy Stage IV Gastric Cancer AJCC v8\|Stage II Pancreatic Cancer AJCC v8\|Stage III Ovarian Cancer AJCC v8\|Stage III Pancreatic Cancer AJCC v8\|Stage III Prostate Cancer AJCC v8\|Stage IV Ovarian Cancer AJCC v8\|Stage IV Pancreatic Cancer AJCC v8\|Stage IVB Prostate Cancer AJCC v8	December 29, 2020	Phase 2
NCT02286687	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Advanced Malignant Neoplasm\|ATM Gene Mutation\|BRCA1 Gene Mutation\|BRCA2 Gene Mutation\|Metastatic Malignant Neoplasm\|PALB2 Gene Mutation\|Recurrent Malignant Neoplasm\|Refractory Malignant Neoplasm	December 22, 2014	Phase 2
NCT04672460	Pfizer	Advanced Solid Tumors\|Solid Tumors\|Ovarian Cancer\|Breast Cancer\|Prostate Cancer\|NSCLC\|Pancreatic Cancer\|Colorectal Cancer	December 21, 2020	Phase 1
NCT04801966	Peter MacCallum Cancer Centre, Australia	Cancer	September 23, 2021	Not Applicable
NCT02392793	St. Jude Children´s Research Hospital\|BioMarin Pharmaceutical\|Alliance Pharma\|Pfizer	Childhood Solid Tumors	March 25, 2015	Phase 1
NCT04598321	Brown University\|Pfizer\|Lifespan	BRCA1 Mutation\|BRCA2 Mutation\|Ovarian Cancer\|Fallopian Tube Cancer\|High Grade Serous Carcinoma	March 29, 2021	Phase 1
NCT04703920	University of Michigan Rogel Cancer Center\|Pfizer\|Acrotech Biopharma Inc.	Metastatic Breast Cancer\|Metastatic Castration-resistant Prostate Cancer\|Metastatic Ovarian Carcinoma	March 4, 2021	Phase 1
NCT04740190	The University of Hong Kong	Recurrent Glioma\|Recurrent Glioblastoma\|Poly ADP Ribose Polymerase (PARP) Inhibitor\|PTEN Gene Inactivation\|IDH Mutation	January 1, 2021	Phase 2
NCT04755868	Yonsei University	TNBC - Triple-Negative Breast Cancer	March 2021	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 108 mg/mL ( 195.46 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8098 mL	9.0490 mL	18.0979 mL
5 mM	0.3620 mL	1.8098 mL	3.6196 mL
10 mM	0.1810 mL	0.9049 mL	1.8098 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013 Sep 15;19(18):5003-15.