MRTX849

SKU: orb1298993

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Description

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.

Research Area

Immunology & Inflammation

Images & Validation

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Key Properties

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CAS Number	2326521-71-3
MW	604.1
Purity	>98%
Formula	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
Target	GTPase
Solubility	Soluble in DMSO (up to 25 mg/ml)

Bioactivity

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Target IC50	Apixaban (rat liver microsomes):7.99 μM\|Apixaban (human liver microsomes):117.40 μM
In Vivo	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.
In Vitro	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.

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Adagrasib

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Compound Identifiers

PubChem CID

138611145 ↗

Key Properties

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No computed properties available.

Protocol Information

Find More Protocols

CAS Number:	2913177-53-2
MW:	1179.86
Formula:	C₆₃H₇₅ClN₁₂O₇S

CAS Number:	2561529-98-2
MW:	720.24
Formula:	C₃₇H₄₃ClFN₇O₅

CAS Number:	2561529-96-0
MW:	662.16
Formula:	C₃₄H₃₇ClFN₇O₄

CAS Number:	2490716-96-4
MW:	656.2
Formula:	C₃₆H₃₉ClFN₇O₂

MRTX849

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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