1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR

JNJ-38877605 

Cat. No.: HY-50683 Purity: 99.95%
Handling Instructions

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.

For research use only. We do not sell to patients.

JNJ-38877605 Chemical Structure

JNJ-38877605 Chemical Structure

CAS No. : 943540-75-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 139 In-stock
Estimated Time of Arrival: December 31
5 mg USD 126 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. IC50 value: 4 nM [1] Target: c-Met in vitro: JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. [1] In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth [2]. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells [3]. in vivo: In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose [3].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (79.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6501 mL 13.2503 mL 26.5006 mL
5 mM 0.5300 mL 2.6501 mL 5.3001 mL
10 mM 0.2650 mL 1.3250 mL 2.6501 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

377.35

Formula

C₁₉H₁₃F₂N₇

CAS No.

943540-75-8

SMILES

FC(F)(C1=NN=C2C=CC(C3=CN(C)N=C3)=NN21)C4=CC5=C(N=CC=C5)C=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.95%

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Product Name:
JNJ-38877605
Cat. No.:
HY-50683
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JNJ-38877605

Cat. No.: HY-50683