Adagrasib (MRTX849) - Moligand™, 10mM in DMSO , GTPase KRas inhibitor, CAS No.2326521-71-3, GTPase KRas inhibitor

CAS: 2326521-71-3 Cat. No.: A408413 分子式: C₃₂H₃₅ClFN₇O₂ 分子量: 604.12 EC番号: 870-640-0

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-Piperazineacetonitrile, 4-[7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

Adagrasib (MRTX849) Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
In vitro

To evaluate the breadth of MRTX849 activity, its effect on cell viability is determined across a panel of 17 KRAS^G12C-mutant and three non-KRAS^G12C-mutant cancer cell lines using 2D (3-day, adherent cells) and 3D (12-day, spheroids) cell growth conditions. MRTX849 potently inhibits cell growth in the vast majority of KRAS^G12C-mutant cell lines with IC50 values ranging between 10 nM and 973 nM in the 2D format and between 0.2 nM and 1042 nM in the 3D format..

In vivo

Rapid tumor regression is observed at the earliest posttreatment tumor measurement and animals in the 30 mg/kg and 100 mg/kg cohorts exhibits evidence of a complete response at study Day 15. Dosing is stopped at study Day 16 and all 4 mice in the 100 mg/kg cohort and 2 out of 7 mice in the 30 mg/kg cohort remains tumor-free through study Day 70..
Cell Data

cell lines：

Concentrations：--

Incubation Time：24 h

Powder Purity:≥99%

Specifications

同義語

2-Piperazineacetonitrile, 4-[7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

GTPase KRas inhibitor

製品の性質

ALogP

5

名前と識別子

異性体SMILES

CN1CCC[C@H]1COC2=NC3=C(CCN(C3)C4=CC=CC5=C4C(=CC=C5)Cl)C(=N2)N6CCN([C@H](C6)CC#N)C(=O)C(=C)F

分子量

604.12

Reaxy-Rn

39485713

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=39485713&ln=

関連ターゲット（人間）

KRAS Tclin GTPase KRas (3 Activities)

Discover Target: KRAS

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)