WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H563541
CAS#: 1246094-78-9 (HCl)
Description: AZD7762 HCl is a checkpoint kinase inhibitor, driving checkpoint abrogation and potentiating DNA-targeted therapies.
Hodoodo Cat#: H563541
Name: AZD7762 HCl
CAS#: 1246094-78-9 (HCl)
Chemical Formula: C17H20ClFN4O2S
Exact Mass: 398.10
Molecular Weight: 398.880
Elemental Analysis: C, 51.19; H, 5.05; Cl, 8.89; F, 4.76; N, 14.05; O, 8.02; S, 8.04
Related CAS #: 860352-01-8 (free base) 1246094-78-9 (HCl)
Synonym: AZD7762 Hydrochloride; AZD7762 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:
| 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 | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.9 | 100.01 | |
| Water | 39.9 | 100.01 |
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: | 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. |
| 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.
