MRTX0902
Based on 2 publication(s) in Google Scholar
MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a Ki of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.67%
- No. CAS: 2654743-22-1
- Fòrmula: C22H24N6O
- Peso molecular:388.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MRTX0902
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
KRAS-SOS1 46 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MKN-1 | IC50 |
29 nM
Compound: 21; MRTX0902
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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
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[PMID: 38430853] |
In Vitro
MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) shows a moderate Clint 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 (Ki=2 nM) over SOS2 and EGFR (both Ki 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 (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) | Vd,ss (L/kg) | T1/2(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.
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Animal Model:Female CD-1 mice[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; twice daily; 1 day
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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 (T1/2 = 1.3 h).
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Animal Model:MIA PaCa-2 xenograft model in mouse[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:Oral gavage; twice daily; 25 days
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Result:Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2654743-22-1
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Appearance Solid
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Peso molecular 388.47
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Fòrmula C22H24N6O
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Color Light yellow to green yellow
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SMILES
C[C@H](C1=C(C(C#N)=CC=C1)C)NC2=NN=C(C)C3=C2C=C(N4CCOCC4)N=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| 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 |
MRTX0902 Related Classifications
HY-145926 Related Classifications
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