2653994-10-4

Name	2-Propen-1-one, 1-[6-[(4S)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-
CAS	2653994-10-4
Molecular Formula	C29H28ClN7O
Molecular Weight	526.04
MOL File	2653994-10-4.mol

Synonyms

(S)-JDQ-443 2-Propen-1-one, 1-[6-[(4S)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-

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Chemical Properties

Boiling point	737.3±60.0 °C(Predicted)
density	1.46±0.1 g/cm3(Predicted)
form	Solid
pka	12.55±0.40(Predicted)
color	Off-white to light yellow

Hazard Information

Uses

(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity[1][2].

in vivo

JDQ443 (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity and inhibits the growth of tumor in a dose-dependent manner in KRAS G12C-mutated CDX models^[2].
JDQ443 (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155^[2].
JDQ443 generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents^[2].

References

[1] LIU BO, et al. PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS. Patent WO2021120890A1.
[2] Weiss A, Lorthiois E, Barys L, et al. Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent and Selective, Covalent Oral Inhibitor of KRASG12C. Cancer Discov. 2022;candisc.0158.2022. DOI:10.1158/2159-8290.CD-22-0158

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

TargetMol Chemicals Inc.

Telephone4008200310 15002144251

Websitehttps://www.targetmol.cn/

Aikon International Limited

Telephone 17714375163

Websitehttp://www.aikonchem.com

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone15000803246 18149758185

Websitehttp://www.caerulumpharma.com/

Zibo Hangyu Biotechnology Development Co., Ltd

Telephone+86-0533-2185556 +8615965530500

Websitehttps://www.chemicalbook.com/manufacturer/hangyu-chemical-25178/

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