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Adagrasib

Catalog No. T8369 CAS 2326521-71-3

Synonyms: MRTX849

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

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Adagrasib, CAS 2326521-71-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 59.00
10 mg	In stock	$ 93.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 553.00
500 mg	In stock	$ 996.00
1 mL * 10 mM (in DMSO)	In stock	$ 94.00

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Purity: 99.9%

Purity: 99.84%

Purity: 99.59%

Purity: 99.10%

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Description	Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.
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. [1] 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. [2]
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. [1] 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. [3]

Synonyms	MRTX849
Molecular Weight	604.12
Formula	C32H35ClFN7O2
CAS No.	2326521-71-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (165.53 mM), Sonication is recommended.

References and Literature

1. Hallin J, et al. The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2020 Jan;10(1):54-71. 2. Fell JB, et al. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer. J Med Chem. 2020 Jul 9;63(13):6679-6693. 3. Zhang Y, et al. Adagrasib, a KRAS G12C inhibitor, reverses the multidrug resistance mediated by ABCB1 in vitro and in vivo. Cell Commun Signal. 2022 Sep 14;20(1):142.

Citations

1. Yang F, Wen Y, Wang C, et al. Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC. European Journal of Medicinal Chemistry. 2022: 114088 2. Yun S D, Scott E, Moghadamchargari Z, et al.2′-Deoxy Guanosine Nucleotides Alter the Biochemical Properties of Ras.Biochemistry.2023

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library GPCR Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Membrane Protein-targeted Compound Library Inhibitor Library Anti-Cancer Active Compound Library FDA-Approved Kinase Inhibitor Library

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Keywords

Adagrasib 2326521-71-3 GPCR/G Protein MAPK Ras inhibit GDP-bound mutant MIA PaCa-2 selective Inhibitor MRTX 849 inactive MRTX-849 state G12C H1373 covalent MRTX849 anti-tumor KRAS cells inhibitor

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