Art. -Nr.: HY-145926

MRTX0902

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a K_i of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma.

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Reinheit: 99.67%
CAS. Nr.: 2654743-22-1
Formel: C₂₂H₂₄N₆O
Molecular Weight:388.47

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MRTX0902 Chemical Structure

CAS. Nr.: 2654743-22-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

KRAS-SOS1

46 nM (IC₅₀)

Alle Ras Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MKN-1	IC₅₀	29 nM Compound: 21; MRTX0902	Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay	[PMID: 38430853]

In Vitro

MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) shows a moderate Cl_int value of 195 mL/min/kg in human liver microsome and a low lipophilicity with cLogP of 3.4^[1].
MRTX0902 displays high selectivity on SOS1 (K_i=2 nM) over SOS2 and EGFR (both K_i values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC₅₀ value of 29 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MRTX0902 (compound 32) (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression^[1].
MRTX0902 (1-3 mg/kg for i.v. or 10-30 mg/kg for p.o.; single dose) exhibits good brain penetrance, low clearance, and high bioavailability^[1].
PK Parameters for MRTX0902 across Species^[1]

Parameter	Route	Dose (mg/kg)	Cl (mL/min/kg)	V_d,ss (L/kg)	T_1/2(iv) (h)	F (%)
Mouse	IV/PO	3/30	4.4	0.28	1.3	69
Rat	IV/PO	1/10	14.6	0.28	0.62	83
Dog	IV/PO	2/10	7.6	0.48	0.86	38

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female CD-1 mice^[1]
Dosage:

50 mg/kg
Administration:

Oral gavage; twice daily; 1 day
Result:

Resulted free drug exposure in the brain as well as the efflux ratio in the Caco-2 assay (ER = 1.5).
Showed short half-life of the compound in mice (T_1/2 = 1.3 h).

Animal Model:

MIA PaCa-2 xenograft model in mouse^[1]
Dosage:

25 mg/kg; 50 mg/kg
Administration:

Oral gavage; twice daily; 25 days
Result:

Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2654743-22-1
Appearance Solid
Molecular Weight 388.47
Formel C₂₂H₂₄N₆O
Color Light yellow to green yellow
SMILES

C[C@H](C1=C(C(C#N)=CC=C1)C)NC2=NN=C(C)C3=C2C=C(N4CCOCC4)N=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Nat Commun

Wild-type KRAS activation drives evasion of interferon-mediated immunity and resistance to immunotherapy in hepatocellular carcinoma. [Abstract]

2025 Nov 11;16(1):9913. PMID: 41219194
bioRxiv

RAS mutation-specific signaling dynamics in response to paralog- and state- selective RAS inhibitors. [Abstract]

2025 Mar 21:2025.02.14.638317. PMID: 40166154

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 12.5 mg/mL (32.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5742 mL

12.8710 mL

25.7420 mL

5 mM

0.5148 mL

2.5742 mL

5.1484 mL

10 mM

0.2574 mL

1.2871 mL

2.5742 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (3.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ketcham JM, et al. Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 2022 Jul 28;65(14):9678-9690. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5742 mL	12.8710 mL	25.7420 mL	64.3550 mL
	5 mM	0.5148 mL	2.5742 mL	5.1484 mL	12.8710 mL
	10 mM	0.2574 mL	1.2871 mL	2.5742 mL	6.4355 mL
	15 mM	0.1716 mL	0.8581 mL	1.7161 mL	4.2903 mL
	20 mM	0.1287 mL	0.6436 mL	1.2871 mL	3.2178 mL
	25 mM	0.1030 mL	0.5148 mL	1.0297 mL	2.5742 mL
	30 mM	0.0858 mL	0.4290 mL	0.8581 mL	2.1452 mL

Keywords

MRTX0902

2 Cited Publications

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MRTX0902

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

KRAS Targeted Compound Library

Publications Citing Use of MedChemExpress (MCE) MRTX0902

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MRTX0902 Related Classifications

Art. -Nr.: HY-145926