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[CAS NO. 1352226-88-0] Ceralasertib

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Catalog:	HY-19323
Brand:	MCE
CAS:	1352226-88-0

Overview

MDL	MFCD28952790
Molecular Weight	412.51
Molecular Formula	C20H24N6O2S
SMILES	O=[S@@](C1(CC1)C2=NC(C3=C4C(NC=C4)=NC=C3)=NC(N5CCOC[C@H]5C)=C2)(C)=N

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

17 Publications Citing Use of MCE

[1]Nat Commun. 2022 Aug 4;13(1):4520.
[2]Nat Commun. 2020 Jan 8;11(1):123.
[3]J Cell Biol. 2021 Feb 1;220(2):e201911025.
[4]Cell Rep. 2022 Nov 15;111716.
[5]Cell Rep. 2020 Sep 1;32(9):108096.
[6]Cell Rep. 2020 Jan 14;30(2):497-509.e4.
[7]EMBO Rep. 2020 Aug 5;21(8):e48920.
[8]PLoS Biol. 2021 Mar 31;19(3):e3001176.
[9]J Exp Clin Cancer Res. 2022 Nov 16;41(1):323.
[10]Cell Death Dis. 2021 Jan 7;12(1):42.
[11]Oncogenesis. 2020 Feb 3;9(2):8.
[12]Mol Cancer Res. 2020 Jan;18(1):91-104.
[13]J Am Heart Assoc. 2021 Aug 3;10(15):e021768.
[14]J Mol Med (Berl). 2019 Aug;97(8):1183-1193.
[15]Phytother Res. 2022.
[16]Transl Oncol. 2021, 101167.
[17]Technische Universität Darmstadt. Department of Biology. 2022 Aug.

Summary

Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC ₅₀ of 1 nM.

IC50 & Target

ATR

1 nM (IC ₅₀ )

PI3Kδ

6.8 μM (IC ₅₀ )

DYRK

10.8 μM (IC ₅₀ )

In Vitro

Ceralasertib (AZD6738) is a potent inhibitor of ATR kinase activity with an IC ₅₀ of 0.001 μM against the isolated enzyme and 0.074 μM against ATR kinase-dependent CHK1 phosphorylation in cells. Ceralasertib (AZD6738) induces cell death and senescence in non-small cell lung cancer (NSCLC) cell lines. Ceralasertib (AZD6738) impairs viability of four Kras mutant cell lines: H23, H460, A549, and H358. , with the lowest GI ₅₀ and greatest maximal inhibition in H460 and H23 cells (1.05 μM, 88.0% and 2.38 μM, 86.2%, respectively). Ceralasertib (AZD6738) potentiates the cytotoxicity of CDDP and NSC 613327 in NSCLC cell lines with intact ATM kinase signaling, and potently synergizes with CDDP in ATM-deficient NSCLC cells ^[1] . Ceralasertib (AZD6738) inhibits human breast cancer cell lines with IC ₅₀ values less than 1 μM using MTT assay. Ceralasertib (AZD6738) induces cell cycle arrest and apoptosis. It downregulates DNA damage response molecules and cell proliferative signaling molecules ^[2] .

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

In Vivo

Daily administration of Ceralasertib (AZD6738) and ATR kinase inhibition for 14 consecutive days is tolerated in mice and enhances the therapeutic efficacy of CDDP in xenograft models. Remarkably, the combination of CDDP and Ceralasertib (AZD6738) resolves ATM-deficient lung cancer xenografts ^[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
NCT02937818	AstraZeneca	Platinum Refractory Extensive-Stage Small Cell Lung Carcinoma	November 28, 2016	Phase 2
NCT05514132	AstraZeneca	Advanced Solid Tumours	September 26, 2022	Phase 1
NCT03801369	OHSU Knight Cancer Institute\|AstraZeneca\|Oregon Health and Science University	Anatomic Stage IV Breast Cancer AJCC v8\|Metastatic Triple-Negative Breast Carcinoma	December 12, 2018	Phase 2
NCT01955668	AstraZeneca\|CLL Consortium	11q-deleted Relapsed+Refractory Chronic Lymphocytic Leukaemia (CLL),\|Prolymphocytic Leukaemia (PLL)\|B Cell Lymphomas	November 2013	Phase 1
NCT03330847	AstraZeneca	Metastatic Triple Negative Breast Cancer	March 7, 2018	Phase 2
NCT03328273	Acerta Pharma BV	Chronic Lymphocytic Leukemia	July 15, 2020	Phase 1
NCT05582538	IFOM, The FIRC Institute of Molecular Oncology\|AstraZeneca	Triple Negative Breast Cancer Metastatic	November 2022	Phase 2
NCT04417062	Dana-Farber Cancer Institute\|Osteosarcoma Institute\|AstraZeneca	Osteosarcoma\|Osteosarcoma Recurrent	November 24, 2020	Phase 2
NCT04065269	Institute of Cancer Research, United Kingdom\|Cancer Research UK\|AstraZeneca	Gynaecological Cancers	November 27, 2019	Phase 2
NCT05450692	AstraZeneca\|Parexel	Advanced or Metastatic Non-Small Cell Lung Cancer	September 15, 2022	Phase 3
NCT02664935	University of Birmingham\|Cancer Research UK\|AstraZeneca\|Pfizer\|Experimental Cancer Medicine Centres\|Mirati Therapeutics Inc.	Non-Small Cell Lung Cancer\|Carcinoma, Squamous Cell\|Adenocarcinoma	May 2015	Phase 2
NCT05469919	AstraZeneca	Advanced Solid Malignancies	June 9, 2022	Phase 1
NCT04090567	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Advanced Breast Carcinoma\|Anatomic Stage III Breast Cancer AJCC v8\|Anatomic Stage IIIA Breast Cancer AJCC v8\|Anatomic Stage IIIB Breast Cancer AJCC v8\|Anatomic Stage IIIC Breast Cancer AJCC v8\|Anatomic Stage IV Breast Cancer AJCC v8\|Germline BRCA1 Gene Mutation\|Germline BRCA2 Gene Mutation\|HER2+Neu Negative\|Metastatic Breast Carcinoma\|Prognostic Stage III Breast Cancer AJCC v8\|Prognostic Stage IIIA Breast Cancer AJCC v8\|Prognostic Stage IIIB Breast Cancer AJCC v8\|Prognostic Stage IIIC Breast Cancer AJCC v8\|Prognostic Stage IV Breast Cancer AJCC v8	July 28, 2020	Phase 2
NCT03787680	University of Michigan Rogel Cancer Center	Prostate Cancer	October 31, 2019	Phase 2
NCT02630199	Samsung Medical Center	Refractory Cancer	December 2015	Phase 1
NCT03022409	AstraZeneca	Head and Neck Squamous Cell Carcinoma	September 18, 2017	Phase 1
NCT03428607	Samsung Medical Center	SCLC	October 17, 2018	Phase 2
NCT03770429	Massachusetts General Hospital\|AstraZeneca	Leukemia\|Myelodysplastic Syndrome	August 5, 2019	Phase 1
NCT03334617	AstraZeneca	Non-Small Cell Lung Cancer	December 18, 2017	Phase 2
NCT03740893	Institute of Cancer Research, United Kingdom\|AstraZeneca	Breast Neoplasm	October 15, 2019	Phase 2
NCT03833440	Assistance Publique Hopitaux De Marseille	Non-small Cell Lung Cancer	October 8, 2019	Phase 2
NCT04298021	Seoul National University Hospital	Bile Duct Cancer\|Chemotherapy Effect	June 25, 2020	Phase 2
NCT04298008	Seoul National University Hospital	Bile Duct Cancer\|Chemotherapy Effect	June 25, 2020	Phase 2
NCT03579316	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Recurrent Fallopian Tube Carcinoma\|Recurrent Ovarian Carcinoma\|Recurrent Primary Peritoneal Carcinoma	December 7, 2018	Phase 2
NCT02223923	Royal Marsden NHS Foundation Trust\|AstraZeneca\|Cancer Research UK\|RM+ICR Biomedical Research Centre	Solid Tumour Refractory to Conventional Treatment	July 2014	Phase 1
NCT05061134	AstraZeneca	Melanoma	August 11, 2022	Phase 2
NCT03669601	CCTU- Cancer Theme\|AstraZeneca\|Cambridge University Hospitals NHS Foundation Trust	Cancer	October 15, 2019	Phase 1
NCT03182634	Institute of Cancer Research, United Kingdom\|Royal Marsden NHS Foundation Trust	Advanced Breast Cancer	December 15, 2016	Phase 2
NCT04699838	Muhammad Furqan\|AstraZeneca\|Big Ten Cancer Research Consortium	Extensive Stage Small Cell Lung Cancer	April 20, 2021	Phase 2
NCT02576444	Joseph Paul Eder\|Dana-Farber Cancer Institute\|Vanderbilt-Ingram Cancer Center\|The Cleveland Clinic\|Yale University	Cancer	November 2015	Phase 2
NCT04704661	National Cancer Institute (NCI)	Advanced Breast Carcinoma\|Advanced Colon Carcinoma\|Advanced Colorectal Carcinoma\|Advanced Endometrial Carcinoma\|Advanced Gastric Carcinoma\|Advanced Gastroesophageal Junction Adenocarcinoma\|Advanced Malignant Solid Neoplasm\|Advanced Salivary Gland Carcinoma\|Anatomic Stage III Breast Cancer AJCC v8\|Anatomic Stage IIIA Breast Cancer AJCC v8\|Anatomic Stage IIIB Breast Cancer AJCC v8\|Anatomic Stage IIIC Breast Cancer AJCC v8\|Anatomic Stage IV Breast Cancer AJCC v8\|Clinical Stage III Gastric Cancer AJCC v8\|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IV Gastric Cancer AJCC v8\|Clinical Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVA Gastric Cancer AJCC v8\|Clinical Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Clinical Stage IVB Gastric Cancer AJCC v8\|Clinical Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|HER2-Positive Breast Carcinoma\|Malignant Hepatobiliary Neoplasm\|Metastatic Breast Carcinoma\|Metastatic Gastroesophageal Junction Adenocarcinoma\|Metastatic Malignant Solid Neoplasm\|Pathologic Stage III Gastric Cancer AJCC v8\|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIA Gastric Cancer AJCC v8\|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIB Gastric Cancer AJCC v8\|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IIIC Gastric Cancer AJCC v8\|Pathologic Stage IV Gastric Cancer AJCC v8\|Pathologic Stage IV Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVA Gastroesophageal Junction Adenocarcinoma AJCC v8\|Pathologic Stage IVB Gastroesophageal Junction Adenocarcinoma AJCC v8\|Prognostic Stage III Breast Cancer AJCC v8\|Prognostic Stage IIIA Breast Cancer AJCC v8\|Prognostic Stage IIIB Breast Cancer AJCC v8\|Prognostic Stage IIIC Breast Cancer AJCC v8\|Prognostic Stage IV Breast Cancer AJCC v8\|Stage III Colon Cancer AJCC v8\|Stage III Colorectal Cancer AJCC v8\|Stage III Major Salivary Gland Cancer AJCC v8\|Stage III Uterine Corpus Cancer AJCC v8\|Stage IIIA Colon Cancer AJCC v8\|Stage IIIA Colorectal Cancer AJCC v8\|Stage IIIA Uterine Corpus Cancer AJCC v8\|Stage IIIB Colon Cancer AJCC v8\|Stage IIIB Colorectal Cancer AJCC v8\|Stage IIIB Uterine Corpus Cancer AJCC v8\|Stage IIIC Colon Cancer AJCC v8\|Stage IIIC Colorectal Cancer AJCC v8\|Stage IIIC Uterine Corpus Cancer AJCC v8\|Stage IIIC1 Uterine Corpus Cancer AJCC v8\|Stage IIIC2 Uterine Corpus Cancer AJCC v8\|Stage IV Colon Cancer AJCC v8\|Stage IV Colorectal Cancer AJCC v8\|Stage IV Major Salivary Gland Cancer AJCC v8\|Stage IV Uterine Corpus Cancer AJCC v8\|Stage IVA Colon Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVA Major Salivary Gland Cancer AJCC v8\|Stage IVA Uterine Corpus Cancer AJCC v8\|Stage IVB Colon Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVB Major Salivary Gland Cancer AJCC v8\|Stage IVB Uterine Corpus Cancer AJCC v8\|Stage IVC Colon Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8\|Stage IVC Major Salivary Gland Cancer AJCC v8\|Unresectable Colorectal Carcinoma\|Unresectable Gastroesophageal Junction Adenocarcinoma\|Unresectable Malignant Solid Neoplasm	March 5, 2021	Phase 1
NCT03462342	University of Pennsylvania\|AstraZeneca	High Grade Serous Carcinoma	March 9, 2018	Phase 2
NCT02264678	AstraZeneca	Adv Solid Malig - H&N SCC, ATM Pro + Def NSCLC, Gastric, Breast and Ovarian Cancer	October 31, 2014	Phase 1\|Phase 2
NCT03780608	Samsung Medical Center	Gastric Adenocarcinoma\|Malignant Melanoma	July 30, 2019	Phase 2
NCT03527147	Acerta Pharma BV\|AstraZeneca	NHL\|DLBCL\|Non-hodgkin´s Lymphoma\|Diffuse Large B Cell Lymphoma	June 19, 2018	Phase 1
NCT03878095	National Cancer Institute (NCI)	Malignant Solid Neoplasm\|Refractory Cholangiocarcinoma\|Refractory Malignant Solid Neoplasm	December 2, 2019	Phase 2
NCT04239014	AstraZeneca\|Parexel	Ovarian Cancer	August 7, 2020	Phase 2
NCT03682289	Rahul Aggarwal\|AstraZeneca\|University of California, San Francisco	Clear Cell Renal Cell Carcinoma\|Locally Advanced Pancreatic Cancer\|Locally Advanced Malignant Solid Neoplasm\|Metastatic Malignant Solid Neoplasm\|Metastatic Renal Cell Carcinoma\|Metastatic Urothelial Carcinoma\|Metastatic Pancreatic Cancer\|Stage III Pancreatic Cancer\|Stage III Renal Cell Cancer\|Stage IV Pancreatic Cancer\|Stage IV Renal Cell Cancer	January 17, 2019	Phase 2
NCT04564027	AstraZeneca	Advanced Solid Tumours	December 1, 2020	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 303.02 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4242 mL	12.1209 mL	24.2418 mL
5 mM	0.4848 mL	2.4242 mL	4.8484 mL
10 mM	0.2424 mL	1.2121 mL	2.4242 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: ≥ 2.08 mg/mL (5.04 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

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

References

[1] Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of CDDP to resolve ATM-deficient non-small cell lung cancer in vivo.
[2] Kim HJ, et al. Anti-tumor activity of the ATR inhibitor AZD6738 in HER2 positive breast cancer cells. Int J Cancer. 2017 Jan 1;140(1):109-119.

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