Olomorasib
Based on 2 publication(s) in Google Scholar
Olomorasib is a potent inhibitor of KRAS G12C. Olomorasib significantly inhibits tumor growth (extracted from patent WO2021118877A1).
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 2771246-13-8
- Formula: C25H19ClF2N4O3S
- Molecular Weight:528.96
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Olomorasib
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Biological Activity
KRAS G12C[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:H358 tumor xenograft mouse model [1]
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Dosage:12.5, 25, 50, 100 mg/kg; 30 mg/kg; single dose
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Administration:
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Result:Exhibited good inhibition of pERK and active KRas after a single dose treatment from 12.5 to 100 mg/kg. 82.2%-90.6 % pERK inhibition, and 73.4%-94% active KRas inhibition were observed at these dose levels.
Showed at 30 mg/kg, 82.6% pERK inhibition observed at 8 hours, and the pERK inhibition decreased to 65.2% at 24 hours. For active KRas, 80.2% inhibition was achieved at 8 hours, and the active KRas inhibition decreased to 54.9% at 24 hours.
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Animal Model:Pancreatic Cancer MiaPaca-2 Xenograft Mouse Model[1]
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Dosage:5, 10, 30 mg/kg; single dose
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Administration:
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Result:Showed dose and time dependent inhibition of pERK and active KRas in MiaPaca-2 model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2771246-13-8
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Appearance Solid
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Molecular Weight 528.96
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Formula C25H19ClF2N4O3S
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Color White to off-white
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SMILES
FC1=CC=[C@]([C@]2=C(F)C=C(C(N3[C@@](CN(CC3)C(C=C)=O)([H])CCO4)=O)C4=C2Cl)C5=C1SC(N)=C5C#N
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Synonyms
KRAS G12C inhibitor 19
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 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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ACS Omega
Application and Cross-Validation of a High-Throughput SPR Method for Characterizing Covalent Binding Ligands. [Abstract]2025 Jul 4;10(27):29637-29646. PMID: 40687013 -
Solvent & Solubility
DMSO : 100 mg/mL (189.05 mM; Need ultrasonic; 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)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 12.5 mg/mL (23.63 mM); Clear solution
This protocol yields a clear solution of ≥ 12.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (125.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 12.5 mg/mL (23.63 mM); Clear solution
This protocol yields a clear solution of ≥ 12.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (125.0 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.
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.
Purity & Documentation
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Data Sheet (280 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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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 1.8905 mL | 9.4525 mL | 18.9050 mL | 47.2626 mL |
| 5 mM | 0.3781 mL | 1.8905 mL | 3.7810 mL | 9.4525 mL | |
| 10 mM | 0.1891 mL | 0.9453 mL | 1.8905 mL | 4.7263 mL | |
| 15 mM | 0.1260 mL | 0.6302 mL | 1.2603 mL | 3.1508 mL | |
| 20 mM | 0.0945 mL | 0.4726 mL | 0.9453 mL | 2.3631 mL | |
| 25 mM | 0.0756 mL | 0.3781 mL | 0.7562 mL | 1.8905 mL | |
| 30 mM | 0.0630 mL | 0.3151 mL | 0.6302 mL | 1.5754 mL | |
| 40 mM | 0.0473 mL | 0.2363 mL | 0.4726 mL | 1.1816 mL | |
| 50 mM | 0.0378 mL | 0.1891 mL | 0.3781 mL | 0.9453 mL | |
| 60 mM | 0.0315 mL | 0.1575 mL | 0.3151 mL | 0.7877 mL | |
| 80 mM | 0.0236 mL | 0.1182 mL | 0.2363 mL | 0.5908 mL | |
| 100 mM | 0.0189 mL | 0.0945 mL | 0.1891 mL | 0.4726 mL |
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