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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 97.13%
- CAS 番号: 1528546-94-2
- 分子式: C25H18F2N4O3
- 分子量:460.43
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保管条件:
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)
生物活性
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1528546-94-2
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性状 Solid
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分子量 460.43
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |