[CAS NO. 195514-63-7] Rimiducid

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PRODUCTS SPECIFICATIONS [195514-63-7]

Catalog

HY-16046

Brand

MCE

CAS

195514-63-7

DESCRIPTION [195514-63-7]

Overview

MDL	MFCD25976784
Molecular Weight	1411.63
Molecular Formula	C78H98N4O20
SMILES	COC1=CC=C(CC[C@@H](OC([C@@H]2CCCCN2C([C@@H](CC)C3=CC(OC)=C(OC)C(OC)=C3)=O)=O)C4=CC=CC(OCC(NCCNC(COC5=CC([C@@H](CCC6=CC=C(OC)C(OC)=C6)OC([C@@H]7CCCCN7C([C@H](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)=CC=C5)=O)=O)=C4)C=C1OC

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

21 Publications Citing Use of MCE

Summary

Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis .

IC50 & Target

EC50: 0.1 nM (FKBP, in HT1080 cells) ^[1]
Fas receptor ^[1]

In Vitro

The human fibrosarcoma line HT1080 is engineered to express stably a fusion protein comprising a myristoylation sequence, two copies of F36V-FKBP, and the human first apoptosis signal (Fas) intracellular domain. Rimiducid (AP1903) elicits potent and dose-dependent apoptotic death of these engineered cells in culture, with an EC ₅₀ of ≈0.1 nM ^[1] . Maximal killing occurred in the presence of 3 to 10 nM Rimiducid (AP1903), and the IC ₅₀ is approximately 0.2 nM. LV′VFas-transduced T lymphocytes expressing high levels of CD25 (top panel) are eliminated by with 66%±7.5% (n=10) efficiency. When cells are examined after CD25 expression returned to basal levels, 63%±4.7% (n=9) killing is observed after Rimiducid treatment ^[2] .

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

In Vivo

Rimiducid (AP1903; i.v.,0.01, 0.1, 1, 10, and 100 mg/kg) elicits a dose-dependent decrease in serum human GH levels, with a half-maximal effective dose of 0.4±0.1 mg/kg ^[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
NCT02849886	Centre Hospitalier Universitaire de Besancon\|Etablissement Français du Sang\|Bellicum Pharmaceuticals	Graft Versus Host Disease\|Hematological Malignancies	April 10, 2019	Phase 1\|Phase 2
NCT03741127	Poseida Therapeutics, Inc.\|California Institute for Regenerative Medicine (CIRM)	Multiple Myeloma	October 29, 2018	Phase 1
NCT02107963	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Sarcoma\|Osteosarcoma\|Neuroblastoma\|Melanoma	February 28, 2014	Phase 1
NCT02744287	Bellicum Pharmaceuticals	Metastatic Castration-resistant Prostate Cancer\|Metastatic Prostate Cancer	November 2016	Phase 1\|Phase 2
NCT04249947	Poseida Therapeutics, Inc.	Prostatic Neoplasms, Castration-Resistant\|Neoplasms by Histologic Type\|Neoplasms, Prostate\|Prostate Cancer\|Metastatic Castration-resistant Prostate Cancer\|Neoplasms\|Prostatic Neoplasms\|Genital Neoplasms, Male\|Urogenital Neoplasms\|Neoplasms by Site\|Prostatic Disease\|Salivary Gland Cancer\|Salivary Gland Tumor\|Adenoid Cystic Carcinoma\|Salivary Duct Carcinoma\|Mucoepidermoid Carcinoma\|Acinic Cell Tumor	February 28, 2020	Phase 1
NCT03016377	UNC Lineberger Comprehensive Cancer Center\|Bellicum Pharmaceuticals	Acute Lymphoblastic Leukemia\|Immune System Diseases\|Immunoproliferative Disorders	March 22, 2012	Phase 1\|Phase 2
NCT01823978	Bellicum Pharmaceuticals	Castrate Resistent Prostate Cancer	April 2013	Phase 1
NCT03056339	M.D. Anderson Cancer Center	B-Lymphoid Malignancies\|Acute Lymphocytic Leukemia\|Chronic Lymphocytic Leukemia\|Non-hodgkin Lymphoma	June 21, 2017	Phase 1\|Phase 2
NCT03301168	Bellicum Pharmaceuticals	Acute Lymphoblastic Leukemia\|Leukemia, Acute Myeloid (AML), Child\|Lymphoma, Non-Hodgkin\|Myelodysplastic Syndromes\|Primary Immune Deficiency Disorder\|Osteopetrosis\|Cytopenia\|Hemoglobinopathy in Children\|Anemia, Aplastic	April 2014	Phase 1\|Phase 2
NCT02477878	Bellicum Pharmaceuticals	Leukemia\|Myelodysplastic Syndromes\|Lymphoma\|Multiple Myeloma\|Hematologic Neoplasms	July 2016	Phase 1
NCT01744223	Bellicum Pharmaceuticals	Acute Lymphoblastic Leukemia\|Acute Myelogenous Leukemia\|Lymphoma\|Myelodysplastic Syndromes	March 2013	Phase 1\|Phase 2
NCT03958656	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Myeloma-Multiple\|Myeloma, Plasma-Cell	June 13, 2019	Phase 1
NCT03459170	Bellicum Pharmaceuticals	Hematologic Malignancy	February 1, 2018	Phase 1
NCT01875237	M.D. Anderson Cancer Center\|Bellicum Pharmaceuticals	Leukemia\|Myeloma\|Myeloproliferative Diseases	December 27, 2013	Phase 1\|Phase 2
NCT02743611	Bellicum Pharmaceuticals	Acute Myeloid Leukemia\|Myelodysplastic Syndrome\|Uveal Melanoma	April 14, 2017	Phase 1\|Phase 2
NCT03288493	Poseida Therapeutics, Inc.\|California Institute for Regenerative Medicine (CIRM)	Multiple Myeloma	September 20, 2017	Phase 1\|Phase 2
NCT02065869	Bellicum Pharmaceuticals	Acute Lymphoblastic Leukemia\|Leukemia, Acute Myeloid (AML), Child\|Lymphoma, Non-Hodgkin\|Myelodysplastic Syndrome\|Primary Immunodeficiency\|Anemia, Aplastic\|Osteopetrosis\|Hemoglobinopathies\|Cytopenia\|Fanconi Anemia\|Diamond Blackfan Anemia\|Thalassemia\|Anemia, Sickle Cell	April 2014	Phase 2
NCT02231710	Bellicum Pharmaceuticals	Primary Immune Deficiency Disorders\|Hemophagocytic Lymphohistiocytosis\|Inherited Bone Marrow Failure Syndrome\|Hemoglobinopathies\|Metabolic Disorders	February 2015	Phase 1
NCT02487459	Bellicum Pharmaceuticals	Hematologic Malignancies	July 2016	Phase 1
NCT03594162	UNC Lineberger Comprehensive Cancer Center\|Bellicum Pharmaceuticals	Acute Lymphoblastic Leukemia\|Immune System Diseases\|Immunoproliferative Disorders
NCT02792114	Memorial Sloan Kettering Cancer Center\|United States Department of Defense	Breast Cancer\|Metastatic HER2-negative Breast	June 2016	Phase 1
NCT03696784	UNC Lineberger Comprehensive Cancer Center\|Bellicum Pharmaceuticals\|The V Foundation	Lymphoma\|Lymphoma, B-Cell\|Immune System Diseases\|Immunoproliferative Disorders\|Lymphatic Diseases	March 12, 2019	Phase 1
NCT01494103	Baylor College of Medicine\|The Methodist Hospital Research Institute\|Center for Cell and Gene Therapy, Baylor College of Medicine	Acute Lymphoblastic Leukemia\|Myelodysplastic Syndrome\|Acute Myeloid Leukemia\|Chronic Myelogenous Leukemia\|Non Hodgkin Lymphoma\|Hemophagocytic Lymphohistiocytosis\|Familial Hemophagocytic Lymphohistiocytosis\|Hemophagocytic Syndrome\|Epstein Barr Virus Infection\|X-linked Lymphoproliferative Disease	November 2011	Phase 1
NCT03699475	Bellicum Pharmaceuticals	Acute Myeloid Leukemia\|Myelodysplastic Syndromes	December 27, 2018	Phase 2\|Phase 3
NCT02786485	Bellicum Pharmaceuticals	Leukemia\|Myelodysplastic Syndromes\|Lymphomas\|Multiple Myeloma\|Other High-risk Hematological Malignancies	May 2016	Phase 1
NCT04960579	Poseida Therapeutics, Inc.	Multiple Myeloma	May 5, 2022	Phase 1
NCT03807063	Fred Hutchinson Cancer Center\|National Cancer Institute (NCI)\|Bellicum Pharmaceuticals	Acute Bilineal Leukemia\|Myelodysplastic+Myeloproliferative Neoplasm\|Myelodysplastic+Myeloproliferative Neoplasm, Unclassifiable\|Myeloproliferative Neoplasm\|Recurrent Acute Biphenotypic Leukemia\|Recurrent Acute Lymphoblastic Leukemia\|Recurrent Acute Myeloid Leukemia\|Recurrent Blastic Plasmacytoid Dendritic Cell Neoplasm\|Recurrent Chronic Lymphocytic Leukemia\|Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Recurrent Chronic Myelomonocytic Leukemia\|Recurrent Myelodysplastic Syndrome	January 2, 2020	Phase 1
NCT03733249	Bellicum Pharmaceuticals	Acute Lymphoblastic Leukemia\|Leukemia, Acute Myeloid (AML), Child\|Lymphoma, Non-Hodgkin\|Myelodysplastic Syndromes\|Primary Immunodeficiency\|Anemia, Aplastic\|Hemoglobinopathies\|Cytopenia\|Fanconi Anemia\|Diamond Blackfan Anemia\|Thalassemia\|Anemia, Sickle Cell	January 2017	Phase 1\|Phase 2
NCT00868595	Bellicum Pharmaceuticals\|M.D. Anderson Cancer Center\|The University of Texas Health Science Center, Houston\|Memorial Hermann Hospital\|Baylor College of Medicine	Castrate Resistant Prostate Cancer (CRPC)	April 2009	Phase 1
NCT03639844	Bellicum Pharmaceuticals	Hurler Syndrome\|Inherited Metabolic Disorder\|Lysosomal Storage Disorder\|Metachromatic Leukodystrophy\|Inborn Errors of Metabolism
NCT05239143	Poseida Therapeutics, Inc.	Breast Cancer\|Ovarian Cancer\|Non Small Cell Lung Cancer\|Colorectal Cancer\|Pancreatic Cancer\|Renal Cell Carcinoma\|Nasopharyngeal Cancer\|Head and Neck Squamous Cell Carcinoma\|Gastric Cancer	February 15, 2022	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years

* The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 35.42 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.7084 mL	3.5420 mL	7.0840 mL
5 mM	0.1417 mL	0.7084 mL	1.4168 mL
10 mM	0.0708 mL	0.3542 mL	0.7084 mL

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

In Vivo:

1.

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

Solubility: ≥ 2.5 mg/mL (1.77 mM); Clear solution

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