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Chemical Structure| 1025720-94-8 Chemical Structure| 1025720-94-8

Structure of BMS 777607
CAS No.: 1025720-94-8

Chemical Structure| 1025720-94-8

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BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, being 40-fold selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.

Synonyms: BMS 817378

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Product Details of BMS 777607

CAS No. :1025720-94-8
Formula : C25H19ClF2N4O4
M.W : 512.89
SMILES Code : O=C(C1=C(OCC)C=CN(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C(Cl)C(N)=NC=C4)C(F)=C3
Synonyms :
BMS 817378
MDL No. :MFCD16495773
InChI Key :VNBRGSXVFBYQNN-UHFFFAOYSA-N
Pubchem ID :24794418

Safety of BMS 777607

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BMS 777607

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human glomerular endothelial cells (HGEC) 1 μM Different time points MSP1 activated RON downstream signaling, resulting in increased phosphorylation of ERK and AKT kinases, expression of Von Willebrand factor, increased cell motility, and re-organization of F-actin. RON kinase inhibitor BMS-777607 significantly reduced RON downstream signaling. PMC5927980
HPDE P5P6e 3 μmol/L 1 hour BMS-777607 completely inhibited phosphorylation in the HPDE P5P6e line, and this inhibition could not be overcome with MSP stimulation. AKT activation was decreased, but there was no effect on the MAPK pathway. PMC4837108
T-47D cells 5 μM 72 hours To study BMS-777607-induced cellular senescence and polyploidy, results showed that BMS-777607 not only induces polyploidy but also causes cellular senescence. PMC5528636
ZR-75-1 cells 5 μM 72 hours To study BMS-777607-induced cellular senescence and polyploidy, results showed that BMS-777607 not only induces polyploidy but also causes cellular senescence. PMC5528636

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Townes sickle cell disease mouse model Subcutaneous injection 150 mg/kg/day Daily from P4 to P16 BMS-777607 significantly reduced glomerular hypertrophy, capillary dilation and congestion, and endothelial injury. PMC5927980

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01721148 Malignant Solid Tumour Phase 1 Completed - -
NCT00605618 Advanced Solid Tumors Phase 1 Phase 2 Completed - Australia, New South Wales ... More >> Local Institution Camperdown, New South Wales, Australia, 2050 Local Institution Kogarah, New South Wales, Australia, 2217 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.20mL

9.75mL

1.95mL

0.97mL

19.50mL

3.90mL

1.95mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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