AZD7762 HCl | CAS#1246094-78-9 | checkpoint kinase inhibitor

MedKoo Cat#: 563541 | Name: AZD7762 HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZD7762 HCl is a checkpoint kinase inhibitor, driving checkpoint abrogation and potentiating DNA-targeted therapies.

Chemical Structure

AZD7762 HCl

CAS#1246094-78-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 563541

Name: AZD7762 HCl

CAS#: 1246094-78-9 (HCl)

Chemical Formula: C17H20ClFN4O2S

Exact Mass: 398.0980

Molecular Weight: 398.88

Elemental Analysis: C, 51.19; H, 5.05; Cl, 8.89; F, 4.76; N, 14.05; O, 8.02; S, 8.04

Price and Availability

Size	Price	Availability	Quantity
25mg	USD 850.00	2 Weeks

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Related CAS #

860352-01-8 (free base) 1246094-78-9 (HCl)

Synonym

AZD7762 Hydrochloride; AZD7762 HCl; AZD 7762 HCl; AZD-7762 HCl;

IUPAC/Chemical Name

(S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide Hydrochloride

InChi Key

WFZBLOIXZRZEDG-YDALLXLXSA-N

InChi Code

InChI=1S/C17H19FN4O2S.ClH/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);1H/t12-;/m0./s1

SMILES Code

O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@@H]3CNCCC3.[H]Cl

Appearance

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

Shelf Life

>3 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

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Potent and selective ATP-competitive inhibitor of Chk1 and Chk2.

In vitro activity:

As shown in Fig. 1a, MTS assay showed that AZD7762 had no significant inhibitory effect on the proliferation of human osteosarcoma cell lines at low concentrations (≤ 200 nmol/L), and AZD7762 inhibited the two cell lines at higher concentrations (> 200 nmol/L). The effect appeared dose-dependent. The IC50 of AZD7762 on HOS and Saos-2 cell lines were 550 nmol/L and 2.3 μmol/L on 24 h, respectively. For further experiments, this study determined the concentration of AZD7762 to be 100 nmol/L based on the results of MTS and according to the referenced literature. At this concentration, AZD7762 had no significant inhibitory effect on the two osteosarcoma cell lines. Reference: Cancer Cell Int. 2019; 19: 195. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6660702/

In vivo activity:

As shown in the orthotopic metastasis model using 4T1 cell line (a mouse breast cancer cell line) carrying luciferase gene, DN10764 treatment significantly suppressed the progression of growth (Figure 6C) as well as lung metastasis (Figure 6D) in a dose-dependent manner. These results were further confirmed in another metastasis model, in which mice were pre-pretreated with DN10764 2 h prior to the injection of MDA-MB-231-luc2-tdTomato cells into the arterial circulation of nude mice via intracardiac injection. As shown in Supplementary Figure S4, compared with vehicle-injected mice, the average bioluminescence at day 43 decreased by 24% or 40% for mice treated with 10 or 20 mg/kg DN1076, respectively. Two dosing regimens (10 mg/kg and 20 mg/kg) did not affect the average animal body weight compared with vehicle groups (Figure 6B and Supplementary Figure S4B). Taken together, these results clearly demonstrated that DN10764 suppressed in vivo tumor progression and metastasis of breast cancer cells. Reference: Oncotarget. 2016 Dec 13; 7(50): 83308–83318. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5347771/

	Solvent	mg/mL	mM
Solubility
	DMSO	39.9	100.01
	Water	39.9	100.01

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 398.88 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.

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

Formulation protocol:

1. Zhu J, Zou H, Yu W, Huang Y, Liu B, Li T, Liang C, Tao H. Checkpoint kinase inhibitor AZD7762 enhance cisplatin-induced apoptosis in osteosarcoma cells. Cancer Cell Int. 2019 Jul 27;19:195. doi: 10.1186/s12935-019-0896-9. PMID: 31372095; PMCID: PMC6660702. 2. Park YH, Kim DK, Kim HW, Kim HS, Lee D, Lee MB, Min KY, Koo J, Kim SJ, Kang C, Kim YM, Kim HS, Choi WS. Repositioning of anti-cancer drug candidate, AZD7762, to an anti-allergic drug suppressing IgE-mediated mast cells and allergic responses via the inhibition of Lyn and Fyn. Biochem Pharmacol. 2018 Aug;154:270-277. doi: 10.1016/j.bcp.2018.05.012. Epub 2018 May 17. PMID: 29777684. 3. Wang L, Wang Y, Chen A, Jalali A, Liu S, Guo Y, Na S, Nakshatri H, Li BY, Yokota H. Effects of a checkpoint kinase inhibitor, AZD7762, on tumor suppression and bone remodeling. Int J Oncol. 2018 Sep;53(3):1001-1012. doi: 10.3892/ijo.2018.4481. Epub 2018 Jul 13. PMID: 30015873; PMCID: PMC6065446. 4. Park JS, Lee C, Kim HK, Kim D, Son JB, Ko E, Cho JH, Kim ND, Nan HY, Kim CY, Yoon S, Lee SH, Choi HG. Suppression of the metastatic spread of breast cancer by DN10764 (AZD7762)-mediated inhibition of AXL signaling. Oncotarget. 2016 Dec 13;7(50):83308-83318. doi: 10.18632/oncotarget.13088. PMID: 27829217; PMCID: PMC5347771.

In vitro protocol:

In vivo protocol:

1. Wang L, Wang Y, Chen A, Jalali A, Liu S, Guo Y, Na S, Nakshatri H, Li BY, Yokota H. Effects of a checkpoint kinase inhibitor, AZD7762, on tumor suppression and bone remodeling. Int J Oncol. 2018 Sep;53(3):1001-1012. doi: 10.3892/ijo.2018.4481. Epub 2018 Jul 13. PMID: 30015873; PMCID: PMC6065446. 2. Park JS, Lee C, Kim HK, Kim D, Son JB, Ko E, Cho JH, Kim ND, Nan HY, Kim CY, Yoon S, Lee SH, Choi HG. Suppression of the metastatic spread of breast cancer by DN10764 (AZD7762)-mediated inhibition of AXL signaling. Oncotarget. 2016 Dec 13;7(50):83308-83318. doi: 10.18632/oncotarget.13088. PMID: 27829217; PMCID: PMC5347771.

1: Cheng H, Merika E, Syrigos KN, Saif MW. Novel agents for the treatment of pancreatic adenocarcinoma. Highlights from the "2011 ASCO Annual Meeting". Chicago, IL, USA; June 3-7, 2011. JOP. 2011 Jul 8;12(4):334-8. Review. PubMed PMID: 21737890. 2: 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. doi: 10.1517/13543784.17.9.1331 . Review. PubMed PMID: 18694366.