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]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C(F)=C)c1cccc2cccc(Cl)c12
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. Read more...
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. Read more...

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.

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MRTX849 (orb1298993)

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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

Purity:	98.00%
CAS Number:	2502156-03-6
MW:	1132.78
Formula:	C₅₉H₇₁ClFN₁₁O₇S

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

MRTX849

Description

Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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MRTX849 (orb1298993)

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