MRTX849

SKU: orb1298993

特色

描述

Adagrasib (MRTX849) is a covalent, orally bioavailable inhibitor that selectively targets the inactive, GDP-bound form of KRAS G12C, blocking its oncogenic signaling. It demonstrates potent anti-tumor activity in both cellular assays and in vivo models, making it a key tool for oncology research targeting KRAS-driven cancers.

研究领域

Immunology & Inflammation

图片与验证

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关键属性

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CAS 号	2326521-71-3
MW	604.1
纯度	>98%
分子式	C₃₂H₃₅ClFN₇O₂
SMILES	CN1CCC[C@H]1COC1=NC(N2CCN([C@@H](CC#N)C2)C(=O)C(F)=C)=C2CCN(CC2=N1)C1=C2C(Cl)=CC=CC2=CC=C1
靶点	GTPase
溶解性	Soluble in DMSO (up to 25 mg/ml)

生物活性

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靶点 IC50	Apixaban (rat liver microsomes):7.99 μM\|Apixaban (human liver microsomes):117.40 μM
体内	METHODS: To assay antitumor activity in vivo, Adagrasib (1-100 mg/kg, 10% Captisol in 10 mM citrate buffer pH 5.0) was administered by gavage to athymic nude mice harboring human pancreatic adenocarcinoma tumor MIA PaCa-2 or human lung adenocarcinoma tumor H358 once daily for 16-22 days. RESULTS: MRTX849 showed dose-dependent antitumor efficacy in a well-tolerated dose range. METHODS: To assay in vivo antitumor activity, Adagrasib (30 mg/kg orally) and paclitaxel (18 mg/kg intraperitoneally) were administered every three days for four weeks to athymic nude mice harboring tumors of ABCB1-mediated MDR xenografts. RESULTS: Tumors were resistant to Adagrasib and paclitaxel alone and did not show significant antitumor effects.Combined treatment with Adagrasib and paclitaxel showed stronger inhibition of tumor growth.
体外	METHODS: Seventeen KRAS G12C mutant and three non-KRAS G12C mutant tumor cells were treated with Adagrasib (0-10 μM) for 3 days, and cell viability was measured in 2D culture using CellTiter-Glo assay. RESULTS: MRTX849 effectively inhibited cell growth in the majority of KRAS G12C mutant cell lines, with IC50 values ranging from 10-973 nM. three non-KRAS G12C mutant cells had IC50 values greater than 1 μM. METHODS: Human lung cells NCI-H358 were treated with Adagrasib for 3 h, and the target inhibitory activity was detected by Cell-Based Phospho-ERK Assay. RESULTS: Adagrasib inhibited the p-ERK level of NCI-H358, and the IC50 was 14 nM.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Adagrasib

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YF135 [orb1983026]
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2913177-53-2
MW:
1179.86
分子式：
C₆₃H₇₅ClN₁₂O₇S
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MRTX849 ethoxypropanoic acid [orb1690774]
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分子式：
C₃₇H₄₃ClFN₇O₅
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MRTX849 acid [orb1690775]
CAS 号：
2561529-96-0
MW:
662.16
分子式：
C₃₄H₃₇ClFN₇O₄
可选规格： 25 mg, 50 mg, 100 mg
MRTX849 analog 24 [orb1690797]
CAS 号：
2490716-96-4
MW:
656.2
分子式：
C₃₆H₃₉ClFN₇O₂
可选规格： 5 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

138611145 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

CAS 号：	2913177-53-2
MW:	1179.86
分子式：	C₆₃H₇₅ClN₁₂O₇S

CAS 号：	2561529-98-2
MW:	720.24
分子式：	C₃₇H₄₃ClFN₇O₅

CAS 号：	2561529-96-0
MW:	662.16
分子式：	C₃₄H₃₇ClFN₇O₄

CAS 号：	2490716-96-4
MW:	656.2
分子式：	C₃₆H₃₉ClFN₇O₂

MRTX849

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

MRTX849-amide-C4-(o)-carborane [orb3211206]

YF135 [orb1983026]

MRTX849 ethoxypropanoic acid [orb1690774]

MRTX849 acid [orb1690775]

MRTX849 analog 24 [orb1690797]

质量保证

化合物标识

关键属性

实验方案信息

可选规格