Elisrasib
Based on 1 Customer Validation
Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRASG12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 2914919-85-8
- Formula: C32H35F6N7O3
- Molecular Weight:679.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
Elisrasib (2-5 days) inhibits the proliferation of MIA-PA-CA-2 and NCI-H358 cells harboring the KRASG12C mutation with IC50 values of 0.44 nM and 0.6 nM[1], respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | AUC0-last | F | Cmax | T1/2 | Vdss | CL |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10.3 mg/kg | p.o. | 1.0 h | 1422 nM·h | 21.9 % | 431 nM | / | / | / |
| Mice[1] | 2.0 mg/kg | i.v. | / | 1297 nM·h | / | / | 1.7 h | 3.9 L/kg | 40.6 mL/min/kg |
| Rat[1] | 2 mg/kg | i.v. | / | 653 nM·h | / | / | 1.9 h | 10.6 L/kg | 71.5 mL/min/kg |
| Rat[1] | 9.8 mg/kg | p.o. | 1.5 h | 995 nM·h | 30.5 % | 220 nM | / | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c Nude treated Mia PaCa-2 cells[1]
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Dosage:10 and 30 mg/kg
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Administration:oral administration; 22 days
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Result:Inhibited the tumor volumes, with TGI of 93.06% and 99.64% by 10 mg/kg and 30 mg/kg, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2914919-85-8
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Appearance Solid
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Molecular Weight 679.66
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Formula C32H35F6N7O3
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Color White to off-white
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SMILES
FC(F)(F)C(C(C)=CC(N)=C1F)=C1[C@@H]2CC3=NC(OC[C@@]45N(CCC5)C[C@@H](C4)F)=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C3CO2
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Synonyms
D3S-001
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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 (147.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (3.68 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 (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.4713 mL | 7.3566 mL | 14.7132 mL | 36.7831 mL |
| 5 mM | 0.2943 mL | 1.4713 mL | 2.9426 mL | 7.3566 mL | |
| 10 mM | 0.1471 mL | 0.7357 mL | 1.4713 mL | 3.6783 mL | |
| 15 mM | 0.0981 mL | 0.4904 mL | 0.9809 mL | 2.4522 mL | |
| 20 mM | 0.0736 mL | 0.3678 mL | 0.7357 mL | 1.8392 mL | |
| 25 mM | 0.0589 mL | 0.2943 mL | 0.5885 mL | 1.4713 mL | |
| 30 mM | 0.0490 mL | 0.2452 mL | 0.4904 mL | 1.2261 mL | |
| 40 mM | 0.0368 mL | 0.1839 mL | 0.3678 mL | 0.9196 mL | |
| 50 mM | 0.0294 mL | 0.1471 mL | 0.2943 mL | 0.7357 mL | |
| 60 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6131 mL | |
| 80 mM | 0.0184 mL | 0.0920 mL | 0.1839 mL | 0.4598 mL | |
| 100 mM | 0.0147 mL | 0.0736 mL | 0.1471 mL | 0.3678 mL |
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