[CAS NO. 1352226-87-9] (S)-Ceralasertib
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PRODUCTS SPECIFICATIONS [1352226-87-9]
Catalog
HY-19323A
Brand
MCE
CAS
1352226-87-9
DESCRIPTION [1352226-87-9]
Overview
| MDL | - |
|---|---|
| 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.
Summary
(S)-Ceralasertib ((S)-AZD6738) is extracted from patent WO2011154737A1, Compound II, exhibits an IC 50 of 2.578 nM [1] . (S)-Ceralasertib is a potent and selective sulfoximine morpholinopyrimidine ATR inhibitor with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. (S)-Ceralasertib is developed improving aqueous solubility and eliminates CYP3A4 time-dependent inhibition [2] .
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05514132 | AstraZeneca |
Advanced Solid Tumours
|
September 26, 2022 | Phase 1 |
| 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 |
| NCT01955668 | AstraZeneca|CLL Consortium |
11q-deleted Relapsed+Refractory Chronic Lymphocytic Leukaemia (CLL),|Prolymphocytic Leukaemia (PLL)|B Cell Lymphomas
|
November 2013 | Phase 1 |
| 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 |
| 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 |
| NCT03669601 | CCTU- Cancer Theme|AstraZeneca|Cambridge University Hospitals NHS Foundation Trust |
Cancer
|
October 15, 2019 | Phase 1 |
| NCT03787680 | University of Michigan Rogel Cancer Center |
Prostate Cancer
|
October 31, 2019 | Phase 2 |
| NCT05450692 | AstraZeneca|Parexel |
Advanced or Metastatic Non-Small Cell Lung Cancer
|
September 15, 2022 | Phase 3 |
| NCT04564027 | AstraZeneca |
Advanced Solid Tumours
|
December 1, 2020 | 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 |
| NCT04417062 | Dana-Farber Cancer Institute|Osteosarcoma Institute|AstraZeneca |
Osteosarcoma|Osteosarcoma Recurrent
|
November 24, 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 |
| NCT03428607 | Samsung Medical Center |
SCLC
|
October 17, 2018 | Phase 2 |
| NCT04699838 | Muhammad Furqan|AstraZeneca|Big Ten Cancer Research Consortium |
Extensive Stage Small Cell Lung Cancer
|
April 20, 2021 | Phase 2 |
| NCT04298008 | Seoul National University Hospital |
Bile Duct Cancer|Chemotherapy Effect
|
June 25, 2020 | Phase 2 |
| NCT04065269 | Institute of Cancer Research, United Kingdom|Cancer Research UK|AstraZeneca |
Gynaecological Cancers
|
November 27, 2019 | Phase 2 |
| NCT03022409 | AstraZeneca |
Head and Neck Squamous Cell Carcinoma
|
September 18, 2017 | Phase 1 |
| NCT02576444 | Joseph Paul Eder|Dana-Farber Cancer Institute|Vanderbilt-Ingram Cancer Center|The Cleveland Clinic|Yale University |
Cancer
|
November 2015 | Phase 2 |
| NCT04298021 | Seoul National University Hospital |
Bile Duct Cancer|Chemotherapy Effect
|
June 25, 2020 | Phase 2 |
| NCT02937818 | AstraZeneca |
Platinum Refractory Extensive-Stage Small Cell Lung Carcinoma
|
November 28, 2016 | 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 |
| NCT05061134 | AstraZeneca |
Melanoma
|
August 11, 2022 | Phase 2 |
| NCT03780608 | Samsung Medical Center |
Gastric Adenocarcinoma|Malignant Melanoma
|
July 30, 2019 | Phase 2 |
| NCT02630199 | Samsung Medical Center |
Refractory Cancer
|
December 2015 | Phase 1 |
| NCT03334617 | AstraZeneca |
Non-Small Cell Lung Cancer
|
December 18, 2017 | Phase 2 |
| NCT03770429 | Massachusetts General Hospital|AstraZeneca |
Leukemia|Myelodysplastic Syndrome
|
August 5, 2019 | Phase 1 |
| NCT03833440 | Assistance Publique Hopitaux De Marseille |
Non-small Cell Lung Cancer
|
October 8, 2019 | Phase 2 |
| NCT03330847 | AstraZeneca |
Metastatic Triple Negative Breast Cancer
|
March 7, 2018 | Phase 2 |
| 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 |
| 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 |
| NCT04239014 | AstraZeneca|Parexel |
Ovarian Cancer
|
August 7, 2020 | Phase 2 |
| NCT03878095 | National Cancer Institute (NCI) |
Malignant Solid Neoplasm|Refractory Cholangiocarcinoma|Refractory Malignant Solid Neoplasm
|
December 2, 2019 | Phase 2 |
| NCT03462342 | University of Pennsylvania|AstraZeneca |
High Grade Serous Carcinoma
|
March 9, 2018 | Phase 2 |
| NCT05469919 | AstraZeneca |
Advanced Solid Malignancies
|
June 9, 2022 | Phase 1 |
| NCT03740893 | Institute of Cancer Research, United Kingdom|AstraZeneca |
Breast Neoplasm
|
October 15, 2019 | Phase 2 |
| NCT03527147 | Acerta Pharma BV|AstraZeneca |
NHL|DLBCL|Non-hodgkin´s Lymphoma|Diffuse Large B Cell Lymphoma
|
June 19, 2018 | 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 |
| NCT03182634 | Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust |
Advanced Breast Cancer
|
December 15, 2016 | 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 : 100 mg/mL ( 242.42 mM ; Need ultrasonic)
Preparing
Stock Solutions
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.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution
*
All of the co-solvents are available by MCE.
References
- [1] By Foote, et al. Morpholinopyrimidines as ATR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. PCT Int. Appl. (2011), WO 2011154737 A1 20111215.
- [2] Foote KM, et al. Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutatedand Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. J Med Chem. 2018 Nov 21;61(22):9889-9907.
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