Calderasib
Based on 1 Customer Validation
Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 2641216-67-1
- Formula: C32H31ClF2N6O4
- Molecular Weight:637.08
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
Biological Activity
Calderasib (MK-1084) (0.01-10 μM, 2 h) inhibits the SOS-catalyzed nucleotide exchange with IC50 of 1.2 nM, inhibits the phosphorylation of ERK1/2 in cell H358 with IC50 of 9 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Calderasib (MK-1084) exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MiaPaCa-2 xenograft models[2]
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Dosage:10-30 mg/kg
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Administration:po for 14 days
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Result:Inhibited tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2641216-67-1
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Appearance Solid
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Molecular Weight 637.08
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Formula C32H31ClF2N6O4
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Color White to off-white
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SMILES
FC1=C2C(OCCOC3=CC=NC(C(C)C)=C3N4C5=NC2=C(Cl)C=C5C(N6[C@@H](C)CN(C(C=C)=O)[C@H](C)C6)=NC4=O)=C(F)C=C1
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Synonyms
MK-1084
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (156.97 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (stored under nitrogen). 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 | 1.5697 mL | 7.8483 mL | 15.6966 mL | 39.2415 mL |
| 5 mM | 0.3139 mL | 1.5697 mL | 3.1393 mL | 7.8483 mL | |
| 10 mM | 0.1570 mL | 0.7848 mL | 1.5697 mL | 3.9242 mL | |
| 15 mM | 0.1046 mL | 0.5232 mL | 1.0464 mL | 2.6161 mL | |
| 20 mM | 0.0785 mL | 0.3924 mL | 0.7848 mL | 1.9621 mL | |
| 25 mM | 0.0628 mL | 0.3139 mL | 0.6279 mL | 1.5697 mL | |
| 30 mM | 0.0523 mL | 0.2616 mL | 0.5232 mL | 1.3081 mL | |
| 40 mM | 0.0392 mL | 0.1962 mL | 0.3924 mL | 0.9810 mL | |
| 50 mM | 0.0314 mL | 0.1570 mL | 0.3139 mL | 0.7848 mL | |
| 60 mM | 0.0262 mL | 0.1308 mL | 0.2616 mL | 0.6540 mL | |
| 80 mM | 0.0196 mL | 0.0981 mL | 0.1962 mL | 0.4905 mL | |
| 100 mM | 0.0157 mL | 0.0785 mL | 0.1570 mL | 0.3924 mL |
Calderasib Related Classifications
HY-162431 Related Classifications
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