Name: Adagrasib (MRTX849)
Brand: Selleck Chemicals
SKU: S8884
Availability: InStock
Rating: 5 (22 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras Aurora Kinase Casein Kinase
Other KRas Inhibitors	RMC-7977 Daraxonrasib (RMC-6236) MRTX1133 Zoldonrasib (RMC-9805) BI-2852 HRS-4642 ARS-1620 BI-3406 BAY-293 ARS-853

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (165.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	604.12	Formula	C₃₂H₃₅ClFN₇O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2326521-71-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	K-Ras(G12C)
In vitro	To evaluate the breadth of Adagrasib (MRTX849) activity, its effect on cell viability is determined across a panel of 17 KRAS^G12C-mutant and three non-KRAS^G12C-mutant cancer cell lines using 2D (3-day, adherent cells) and 3D (12-day, spheroids) cell growth conditions. This compound potently inhibits cell growth in the vast majority of KRAS^G12C-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..
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 of Adagrasib (MRTX849) exhibit 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 remain tumor-free through study Day 70..
References	[1] https://pubmed.ncbi.nlm.nih.gov/31658955-the-kras-g12c-inhibitor-mrtx849-provides-insight-toward-therapeutic-susceptibility-of-kras-mutant-cancers-in-mouse-models-and-patients/?from_single_result=The+KRASG12C+Inhibitor%2C+MRTX849%2C+Provides+Insight+Toward+Therapeutic+Susceptibility+of+KRAS+Mutant+Cancers+in+Mouse+Models+and+Patients

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05853575	Recruiting	Advanced Cancer\|Metastatic Cancer\|Malignant Neoplasm of Lung	Mirati Therapeutics Inc.	February 1 2024	Phase 2
NCT06039384	Recruiting	Advanced Solid Tumors	Incyte Corporation\|Mirati Therapeutics Inc.	December 28 2023	Phase 1
NCT05924152	Completed	Healthy Adults	Mirati Therapeutics Inc.	June 29 2023	Phase 1
NCT05868356	Completed	Healthy Adults	Mirati Therapeutics Inc.	June 1 2023	Phase 1
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

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Adagrasib (MRTX849) KRAS G12C inhibitor

Chemical Structure

Molecular Weight: 604.12