AZD-7762
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MedKoo CAT#: 200311

CAS#: 860352-01-8 (free base)

Description: AZD-7762 is a synthetic small molecule inhibitor of checkpoint kinases (Chks) with potential chemosensitizing activity. AZD7762 binds to and inhibits Chks, which may prevent cell cycle arrest and subsequent nucleotide excision repair in DNA-damaged tumor cells, resulting in tumor cell apoptosis. This agent may enhance the cytotoxicity of DNA-damaging agents. Chks are protein kinases that regulate either G1/S or G2/M transitions in the cell cycle. In the presence of DNA damage or incomplete DNA replication, Chks become activated and initiate cell cycle arrest to allow DNA repair or the completion of DNA replication.


Chemical Structure

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AZD-7762
CAS# 860352-01-8 (free base)

Theoretical Analysis

MedKoo Cat#: 200311
Name: AZD-7762
CAS#: 860352-01-8 (free base)
Chemical Formula: C17H19FN4O2S
Exact Mass: 362.12127
Molecular Weight: 362.42
Elemental Analysis: C, 56.34; H, 5.28; F, 5.24; N, 15.46; O, 8.83; S, 8.85

Size Price Shipping out time Quantity
100mg USD 550 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1950 2 Weeks
1g USD 2950 2 Weeks
2g USD 5450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-07. Prices are subject to change without notice.

AZD-7762 purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Related CAS #: 860352-01-8 (free base)   1246094-78-9 (HCl)    

Synonym: AZD7762; AZD 7762; AZD-7762.

IUPAC/Chemical Name: (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide

InChi Key: IAYGCINLNONXHY-LBPRGKRZSA-N

InChi Code: InChI=1S/C17H19FN4O2S/c18-11-4-1-3-10(7-11)14-8-13(22-17(19)24)15(25-14)16(23)21-12-5-2-6-20-9-12/h1,3-4,7-8,12,20H,2,5-6,9H2,(H,21,23)(H3,19,22,24)/t12-/m0/s1

SMILES Code: O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@@H]3CNCCC3

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Certificate of Analysis:

Safety Data Sheet (SDS):

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 362.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Mitchell JB, Choudhuri R, Fabre K, Sowers AL, Citrin D, Zabludoff SD, Cook JA. In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762. Clin Cancer Res. 2010 Apr 1;16(7):2076-84. Epub 2010 Mar 16. PubMed PMID: 20233881; PubMed Central PMCID: PMC2851146.

2: McNeely S, Conti C, Sheikh T, Patel H, Zabludoff S, Pommier Y, Schwartz G, Tse A. Chk1 inhibition after replicative stress activates a double strand break response mediated by ATM and DNA-dependent protein kinase. Cell Cycle. 2010 Mar;9(5):995-1004. Epub 2010 Mar 14. PubMed PMID: 20160494.

3: Goteti K, Garner CE, Utley L, Dai J, Ashwell S, Moustakas DT, Gönen M, Schwartz GK, Kern SE, Zabludoff S, Brassil PJ. Preclinical pharmacokinetic/pharmacodynamic models to predict synergistic effects of co-administered anti-cancer agents. Cancer Chemother Pharmacol. 2010 Jul;66(2):245-54. Epub 2009 Oct 16. PubMed PMID: 19841922.

4: Wagner JM, Karnitz LM. Cisplatin-induced DNA damage activates replication checkpoint signaling components that differentially affect tumor cell survival. Mol Pharmacol. 2009 Jul;76(1):208-14. Epub 2009 Apr 29. PubMed PMID: 19403702; PubMed Central PMCID: PMC2701464.

5: Zabludoff SD, Deng C, Grondine MR, Sheehy AM, Ashwell S, Caleb BL, Green S, Haye HR, Horn CL, Janetka JW, Liu D, Mouchet E, Ready S, Rosenthal JL, Queva C, Schwartz GK, Taylor KJ, Tse AN, Walker GE, White AM. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol Cancer Ther. 2008 Sep;7(9):2955-66. PubMed PMID: 18790776.

6: Ashwell S, Janetka JW, Zabludoff S. Keeping checkpoint kinases in line: new selective inhibitors in clinical trials. Expert Opin Investig Drugs. 2008 Sep;17(9):1331-40. Review. PubMed PMID: 18694366.



Additional Information

AZD7762, a potent ATP-competitive checkpoint kinase inhibitor in clinical trials. AZD7762 has been profiled extensively in vitro and in vivo in combination with DNA-damaging agents and has been shown to potentiate response in several different settings where inhibition of checkpoint kinase results in the abrogation of DNA damage-induced cell cycle arrest. Dose-dependent potentiation of antitumor activity, when AZD7762 is administered in combination with DNA-damaging agents, has been observed in multiple xenograft models with several DNA-damaging agents, further supporting the potential of checkpoint kinase inhibitors to enhance the efficacy of both conventional chemotherapy and radiotherapy and increase patient response rates in a variety of settings. (source: Mol Cancer Ther. 2008 Sep;7(9):2955-66.).
(source: Mol Cancer Ther. 2008 Sep;7(9):2955-66.).