MET kinase-IN-2
Based on 1 Customer Validation
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
For research use only. We do not sell to patients.
- Purity: 98.08%
- CAS No.: 2101241-90-9
- Formula: C33H27FN4O4
- Molecular Weight:562.59
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
4.2 μM
Compound: 20j
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Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 32113049] |
| MKN-45 | IC50 |
2.9 μM
Compound: 20j
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Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 32113049] |
| NCI-H460 | IC50 |
3.6 μM
Compound: 20j
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Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 32113049] |
MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM[1].
MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2，CL, and F% values are 1.5 µg/mL, 10.7 µg•h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-6 weeks old Female nude mice (U-87 MG xenograft model)[1]
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Dosage:3, 6, 12.5, 37.5 mg/kg
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Administration:P.o.; 7 days per week for 3 weeks
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Result:Induced dose-dependent tumor growth inhibition.
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Animal Model:Male SD rats[1]
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Dosage:5 mg/kg
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Administration:P.o. (Pharmacokinetic Analysis)
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Result:Displayed favorable overall PK profiles, with maximal plasma concentration (Cmax=1.5 µg/mL, 5-fold higher to that of IV), plasma exposure (AUC0-∞=10.7 µg•h/mL, 9.7-fold higher to that of IV), half-life (T1/2=4.9 h, 4.9-fold longer to that of IV), total clearance CL (0.5 L/h/kg; 10-fold lower to that of IV), and oral bioavailability (F=32%, 2.7-fold higher to that of IV) after oral dose of 5 mg/kg (10 mg/kg for IV).
Chemical Information
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CAS No. 2101241-90-9
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Appearance Solid
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Molecular Weight 562.59
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Formula C33H27FN4O4
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Color Off-white to light yellow
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SMILES
O=C1C(C2=CC=CC=C2)=CNC3=C1C(NC4=CC=C(OC5=CC=NC6=CC(OCC(C)(O)C)=CC=C56)C(F)=C4)=NC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (177.75 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 (protect from light, 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 (protect from light, 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 (272 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 (protect from light, 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 |
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| DMSO | 1 mM | 1.7775 mL | 8.8875 mL | 17.7749 mL | 44.4373 mL |
| 5 mM | 0.3555 mL | 1.7775 mL | 3.5550 mL | 8.8875 mL | |
| 10 mM | 0.1777 mL | 0.8887 mL | 1.7775 mL | 4.4437 mL | |
| 15 mM | 0.1185 mL | 0.5925 mL | 1.1850 mL | 2.9625 mL | |
| 20 mM | 0.0889 mL | 0.4444 mL | 0.8887 mL | 2.2219 mL | |
| 25 mM | 0.0711 mL | 0.3555 mL | 0.7110 mL | 1.7775 mL | |
| 30 mM | 0.0592 mL | 0.2962 mL | 0.5925 mL | 1.4812 mL | |
| 40 mM | 0.0444 mL | 0.2222 mL | 0.4444 mL | 1.1109 mL | |
| 50 mM | 0.0355 mL | 0.1777 mL | 0.3555 mL | 0.8887 mL | |
| 60 mM | 0.0296 mL | 0.1481 mL | 0.2962 mL | 0.7406 mL | |
| 80 mM | 0.0222 mL | 0.1111 mL | 0.2222 mL | 0.5555 mL | |
| 100 mM | 0.0178 mL | 0.0889 mL | 0.1777 mL | 0.4444 mL |
MET kinase-IN-2 Related Classifications
HY-131065 Related Classifications
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