Home Cell Cycle Ras inhibitor Adagrasib (MRTX849) For research use only.

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.

Adagrasib (MRTX849) Chemical Structure

Adagrasib (MRTX849) Chemical Structure

CAS: 2326521-71-3

Selleck's Adagrasib (MRTX849) has been cited by 10 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description 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.
Targets
K-Ras(G12C) [1]
In vitro
In vitro

To evaluate the breadth of MRTX849 activity, its effect on cell viability is determined across a panel of 17 KRASG12C-mutant and three non-KRASG12C-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 KRASG12C-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.[1].
Cell Research Cell lines MIA PaCa-2, H1373, H358, H2122, SW1573, H2030, KYSE-410 cells (G12C); H1299 (WT); A549 (G12S), HCT116 (G13D) cells
Concentrations --
Incubation Time 24 h
Method

All cell lines were maintained at 37 ℃ in a humidified incubator at 5% CO2 and were periodically checked for mycoplasma. CellTiter-Glo assay to evaluate cell viability performed on seven KRAS G12C-mutant cell lines and three non-KRAS G12C-mutant cell lines cells grown in 2D tissue culture conditions in a 3-day assay or 3D conditions using 96-well, ULA plates in a 12-day assay.
In Vivo
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.[1].
Animal Research Animal Models MIA PaCa-2 model
Dosages 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06039384 Recruiting Advanced Solid Tumors Incyte Corporation|Mirati Therapeutics Inc. December 28 2023 Phase 1
NCT05924152 Recruiting Healthy Adults Mirati Therapeutics Inc. June 29 2023 Phase 1
NCT05868356 Not yet recruiting Healthy Adults Mirati Therapeutics Inc. May 26 2023 Phase 1
NCT05853575 Recruiting Advanced Cancer|Metastatic Cancer|Malignant Neoplasm of Lung Mirati Therapeutics Inc. April 5 2023 Phase 2
NCT05375994 Recruiting Non Small Cell Lung Cancer|KRAS Activating Mutation|Advanced Cancer|Metastatic Cancer|Malignant Neoplasm of Lung|Malignant Neoplastic Disease Verastem Inc.|Mirati Therapeutics Inc. August 1 2022 Phase 1|Phase 2
NCT04685135 Active not recruiting Metastatic Non Small Cell Lung Cancer|Advanced Non Small Cell Lung Cancer Mirati Therapeutics Inc. April 1 2021 Phase 3

Chemical lnformation & Solubility

Molecular Weight 604.12 Formula

C32H35ClFN7O2
CAS No. 2326521-71-3 SDF --
Smiles CN1CCCC1COC2=NC3=C(CCN(C3)C4=CC=CC5=C4C(=CC=C5)Cl)C(=N2)N6CCN(C(C6)CC#N)C(=O)C(=C)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (165.53 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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