KRAS inhibitor-10
Based on 1 Customer Validation
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 2578876-75-0
- Formula: C30H37N3O5
- Molecular Weight:519.63
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Storage: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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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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Lactylation Compound Library
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KRAS Targeted Compound Library
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Biological Activity
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KRas G12C |
KRAS inhibitor-10 (0.1-50 µΜ; 72 hours) has antiproliferative effects in KRas mutant tumor cells, KRAS inhibitor-10 is against A549 (lung carcinoma cell line bearing KRasG12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRasG12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRasG12D oncogenic mutation) and RPMI (myeloma cell line bearing KRasG12A oncogenic mutation) cell proliferation with IC50 values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively[1].KRAS inhibitor-10 (0-1 μM, 7 days) is against cell viability in a 3D CellTiter-GloTM cell viability assay for NIH-H358 cell, the IC50 value is 0.413 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice[1]
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Dosage:20 mg/kg
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Administration:Oral administration; 20 mg/kg; BID; 27 days
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Result:Decreased tumor volume and exhibited anti-tumor effects in the bearing mice.
Chemical Information
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CAS No. 2578876-75-0
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Appearance Solid
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Molecular Weight 519.63
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Formula C30H37N3O5
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Color White to off-white
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SMILES
O=C(N1C(C2=CC=C(OC)C=C2C)C3=C(C=C(OC)C(OCCC4=CC=C(OC)C(N)=C4)=C3)CC1)NCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (192.44 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: ≥ 2.5 mg/mL (4.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9244 mL | 9.6222 mL | 19.2445 mL | 48.1112 mL |
| 5 mM | 0.3849 mL | 1.9244 mL | 3.8489 mL | 9.6222 mL | |
| 10 mM | 0.1924 mL | 0.9622 mL | 1.9244 mL | 4.8111 mL | |
| 15 mM | 0.1283 mL | 0.6415 mL | 1.2830 mL | 3.2074 mL | |
| 20 mM | 0.0962 mL | 0.4811 mL | 0.9622 mL | 2.4056 mL | |
| 25 mM | 0.0770 mL | 0.3849 mL | 0.7698 mL | 1.9244 mL | |
| 30 mM | 0.0641 mL | 0.3207 mL | 0.6415 mL | 1.6037 mL | |
| 40 mM | 0.0481 mL | 0.2406 mL | 0.4811 mL | 1.2028 mL | |
| 50 mM | 0.0385 mL | 0.1924 mL | 0.3849 mL | 0.9622 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3207 mL | 0.8019 mL | |
| 80 mM | 0.0241 mL | 0.1203 mL | 0.2406 mL | 0.6014 mL | |
| 100 mM | 0.0192 mL | 0.0962 mL | 0.1924 mL | 0.4811 mL |
KRAS inhibitor-10 Related Classifications
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