BMS 777607

SKU: orb1305149

Description

BMS-777607 is a potent small molecule inhibitor targeting the receptor tyrosine kinases c-Met, Axl, Ron, and Tyro3. It has demonstrated activity in preclinical research, including in vitro cell-based assays and in vivo xenograft models, for studying various solid tumors.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1025720-94-8
• MW: 512.89
• Purity: >99.99% (May vary between batches)
• Formula: C₂₅H₁₉ClF₂N₄O₄
• SMILES: CCOc1ccn(-c2ccc(F)cc2)c(=O)c1C(=O)Nc1ccc(Oc2ccnc(N)c2Cl)c(F)c1
• Target: c-Met/HGFR,TAM Receptor
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.9 mM);DMSO:44 mg/mL (85.79 mM)

Bioactivity

• Target IC50:
  Tyro3:4.3 nM|RON:1.8 nM|MET:3.9 nM|Axl:1.1 nM
• In Vivo:
  BMS-777607 did not affect tumor cell growth much, it inhibited hepatocyte growth factor-induced cell dispersal in PC-3 and DU145 cells, it also dose-dependently inhibited cell migration and invasion (IC50<0.1 μM).BMS-777607 is a selective ATP-competitive Met kinase inhibitor, it has strong inhibition of c-Met autophosphorylation, the IC50 of GTL-16 cell lysates is 20 nM, and it inhibits Met-driven tumor cell lines such as GTL-16 cell line, H1993 and U87 cells. , with an IC50 of 20 nM for GTL-16 cell lysates and selective inhibition of proliferation of Met-driven tumor cell lines such as GTL-16 cell line, H1993 and U87 cells. In DU145 prostate cancer cells, BMS-777607 inhibited c-Met autophosphorylation induced by hepatocyte growth factor (HGF) (IC50<1 nM).BMS-777607 (1 μM) treatment for 24 h effectively inhibited KHT cell dispersal, motility, and invasion, which was associated with the inhibition of the MET gene, and had a certain effect on cell proliferation and colony formation. This is related to the inhibition of MET gene and has certain effects on cell proliferation and colony formation. In highly metastatic murine KHT cells, BMS-777607 (10 μM) treatment for 2 h effectively cleared the level of autophosphorylated c-Met (IC50: 10 nM) without affecting the whole c-Met, which dose-dependently inhibited downstream signaling molecules including ERK, Akt, p70S6K and S6.
• In Vitro:
  BMS-777607 did not affect tumor cell growth much, it inhibited hepatocyte growth factor-induced cell dispersal in PC-3 and DU145 cells, it also dose-dependently inhibited cell migration and invasion (IC50<0.1 μM).BMS-777607 is a selective ATP-competitive Met kinase inhibitor, it has strong inhibition of c-Met autophosphorylation, the IC50 of GTL-16 cell lysates is 20 nM, and it inhibits Met-driven tumor cell lines such as GTL-16 cell line, H1993 and U87 cells. , with an IC50 of 20 nM for GTL-16 cell lysates and selective inhibition of proliferation of Met-driven tumor cell lines such as GTL-16 cell line, H1993 and U87 cells. In DU145 prostate cancer cells, BMS-777607 inhibited c-Met autophosphorylation induced by hepatocyte growth factor (HGF) (IC50<1 nM).BMS-777607 (1 μM) treatment for 24 h effectively inhibited KHT cell dispersal, motility, and invasion, which was associated with the inhibition of the MET gene, and had a certain effect on cell proliferation and colony formation. This is related to the inhibition of MET gene and has certain effects on cell proliferation and colony formation. In highly metastatic murine KHT cells, BMS-777607 (10 μM) treatment for 2 h effectively cleared the level of autophosphorylated c-Met (IC50: 10 nM) without affecting the whole c-Met, which dose-dependently inhibited downstream signaling molecules including ERK, Akt, p70S6K and S6.
• Cell Research:
  KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 ml pipette tip followed by treated with BMS-777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μm pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37 °C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5 × 103/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted. (Only for Reference)

Storage & Handling

• Storage: keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS 777607, BMS 817378, BMS777607, BMS-777607, BMS817378, BMS-817378, AXL, Axl, cMet, c-Met, c-Met/HGFR, cMet/HGFR, Mer, HGFR, Met, Inhibitor, inhibit, RON, TAMReceptor, TAM Receptor, Tyro3

Compound Identifiers

PubChem CID

24794418