Art. -Nr.: HY-114356

BPI-9016M

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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.

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Reinheit: 97.13%
CAS. Nr.: 1528546-94-2
Formel: C₂₅H₁₈F₂N₄O₃
Molecular Weight:460.43

Speicherung:

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)

BPI-9016M Chemical Structure

CAS. Nr.: 1528546-94-2

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]^[2].

In Vitro

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.

Cell Proliferation Assay^[2]

Cell Line:

A549 and H1299 cells
Concentration:

6.3, 12.5, 25 μM
Incubation Time:

2 weeks
Result:

Colony formation was significantly inhibited in a dose-dependent manner.

Cell Cycle Analysis^[2]

Cell Line:

A549 and H1299 cells
Concentration:

12.5, 25, 50 μM
Incubation Time:

24 hours
Result:

Induced accumulation of more tumor cells in the G1 phase.

In Vivo

BPI-9016M (60 mg/kg; p.o.; daily for 16 or 12 days) dramatically restrains tumor growth in PDX xenografts in NOD/SCID mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD/SCID mice^[2]
Dosage:

60 mg/kg
Administration:

p.o.; daily for 16 or 12 days
Result:

Dramatically restrained tumor growth in PDX xenografts in NOD/SCID mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1528546-94-2
Appearance Solid
Molecular Weight 460.43
Formel C₂₅H₁₈F₂N₄O₃
Color Light yellow to brown
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1719 mL

10.8594 mL

21.7188 mL

5 mM

0.4344 mL

2.1719 mL

4.3438 mL

10 mM

0.2172 mL

1.0859 mL

2.1719 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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BPI-9016M

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BPI-9016M

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BPI-9016M Related Classifications

HY-114356 Related Classifications