JNJ-38877605 Chemical Structure
Inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib (PF02341066) inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).
PHA-665752 is c-Met inhibitor with an IC50 of 9 nM and Ki of 4 nM.
SU11274 is a c-Met inhibitor (IC50 at 0.012μM).
PF-04217903 is a MET inhibitor with an IC50 from 3.1 nM to142 nM.
Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively.
SGX-523 is an exquisitely selective MET receptor tyrosine kinase inhibitor with an IC50 of 4 nM.
XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.
MP-470 (Amuvatinib) is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM.
AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.
MGCD-265 is a multi-targeted kinase inhibitor, which targets the c-MET, VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron receptor tyrosine kinases.
JNJ-38877605 is an orally bioavailable, highly specific MET inhibitor (selective over other 229 kinases tested). This agent inhibits c-MET and Phospho-MET with IC50 at 4 nmol/L and 50 nmol/L, respectively. In addition, JNJ-38877605 induces regression of U87-MG xenografts in vivo. [1]
| Molecular Weight (WM): | 377.35 |
|---|---|
| Formula: | C19H13F2N7 |
| CAS No.: | 943540-75-8 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥76mg/mL |
| Water <1mg/mL | |
| Ethanol ≥2mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

| Inducers of EMT. (A) Expression of Hgf, Egf, and Tgfb1 genes in RETAAD tumors analyzed by qRT-PCR. Hgf and Tgfb1 are preferentially expressed in PMN-MDSC, while Egf is preferentially expressed in tumor cells. Data are from four individual experiments using sorted fractions of PMNMDSC and melanoma cells. Bars represent mean 6 SD. (B) NBT-II cells (100 cells per well) were plated for 4 d to allow for colony growth and were pretreated for 24 h with inhibitors before the addition of PMN-MDSC. After co-culture with PMN-MDSCs in the presence of inhibitors, cells were fixed and stained with anti-rat desmoplakin. Green, Desmoplakin; red, H2b (nuclear stain). PD153035 – EGFR inhibitor, JNJ38877605 – c-met (HGFR) inhibitor, and SB525334 – TGF-bR1 inhibitor. Images are representative of three independent experiments. |
Data from [PLoS Biology 2011.September;9:e1001162 ] JNJ-38877605 purchased from Selleck

After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of JNJ-38877605 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
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After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of JNJ-38877605 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
Data independently produced by Dr.Zhang of Tianjin Medical University JNJ-38877605 purchased from Selleck
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