BPI-9016M
Based on 1 Customer Validation
BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 97.13%
- CAS No.: 1528546-94-2
- Formule: C25H18F2N4O3
- Masse moléculaire:460.43
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Kinase Inhibitor Library
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Protein Tyrosine Kinase Compound Library
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Activité biologique
BPI-9016M (6.3-25 μM; 2 weeks) inhibited cell proliferation[2].
BPI-9016M (12.5-50 μM; 24 hpurs) induces accumulation of more tumor cells in the G1 phase[2].
BPI-9016M (3.1-50 μM) reduces expression of c-Met, p-c-Met, p-AKT and p-ERK in the H1299 and A549 cells in a dose-dependent manner[2].
The IC50 of BPI-9016M in several lung adenocarcinoma cell lines ( A549, H1299, H1650, H1975, HCC827, and PC-9 cells) as well as in primary lung adenocarcinoma cells are ranged from 5.3 μM to 27.1 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and H1299 cells
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Concentration:6.3, 12.5, 25 μM
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Incubation Time:2 weeks
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Result:Colony formation was significantly inhibited in a dose-dependent manner.
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Cell Line:A549 and H1299 cells
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Concentration:12.5, 25, 50 μM
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Incubation Time:24 hours
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Result:Induced accumulation of more tumor cells in the G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice[2]
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Dosage:60 mg/kg
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Administration:p.o.; daily for 16 or 12 days
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Result:Dramatically restrained tumor growth in PDX xenografts in NOD/SCID mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1528546-94-2
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Appearance Solid
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Masse moléculaire 460.43
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Formule C25H18F2N4O3
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Color Light yellow to brown
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SMILES
O=C(C1=CNC=C(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NCC5)=NC=C4)C(F)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 100 mg/mL (217.19 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
[1]. Zhang P, et al. BPI-9016M, a c-Met inhibitor, suppresses tumor cell growth, migration and invasion of lung adenocarcinoma via miR203-DKK1. Theranostics. 2018 Nov 12;8(21):5890-5902. [Content Brief]
[2]. Hu X, et al. First-in-human phase I study of BPI-9016M, a dual MET/Axl inhibitor, in patients with non-small cell lung cancer.J Hematol Oncol. 2020 Jan 16;13(1):6. [Content Brief]
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 (sealed storage, away from moisture and light). 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 | 2.1719 mL | 10.8594 mL | 21.7188 mL | 54.2971 mL |
| 5 mM | 0.4344 mL | 2.1719 mL | 4.3438 mL | 10.8594 mL | |
| 10 mM | 0.2172 mL | 1.0859 mL | 2.1719 mL | 5.4297 mL | |
| 15 mM | 0.1448 mL | 0.7240 mL | 1.4479 mL | 3.6198 mL | |
| 20 mM | 0.1086 mL | 0.5430 mL | 1.0859 mL | 2.7149 mL | |
| 25 mM | 0.0869 mL | 0.4344 mL | 0.8688 mL | 2.1719 mL | |
| 30 mM | 0.0724 mL | 0.3620 mL | 0.7240 mL | 1.8099 mL | |
| 40 mM | 0.0543 mL | 0.2715 mL | 0.5430 mL | 1.3574 mL | |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4344 mL | 1.0859 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9050 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2715 mL | 0.6787 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5430 mL |
BPI-9016M Related Classifications
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