JNJ-38877605

Catalog No.S1114 Batch:S111401

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Technical Data

Formula

C19H13F2N7
Molecular Weight 377.35 CAS No. 943540-75-8
Solubility (25°C)* In vitro DMSO 50 mg/mL (132.5 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

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. Phase 1.
Targets
c-Met [1]
4 nM
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]

Protocol (from reference)

Animal Study:[3]
  • Animal Models

    GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.

  • Dosages

    ≤40 mg/kg/day

  • Administration

    Administered via p.o.

Customer Product Validation

Data from [PLoS One, 2012, 7, e44937]

Data from [PLoS One, 2012, 7, e44937]

Data from [PLoS One, 2012, 7, e44937]

Data from [PLoS Biol, 2011, 9, e1001162 ]

Selleck's JNJ-38877605 has been cited by 54 publications

The Receptor Tyrosine Kinase c-Met Promotes Lipid Accumulation in 3T3-L1 Adipocytes [ Int J Mol Sci, 2023, 24(9)8086] PubMed: 37175792
The Receptor Tyrosine Kinase c-Met Promotes Lipid Accumulation in 3T3-L1 Adipocytes [ Int J Mol Sci, 2023, 24(9)8086] PubMed: 37175792
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306
Precision Combination Therapies Based on Recurrent Oncogenic Coalterations [ Cancer Discov, 2022, 12(6):1542-1559] PubMed: 35412613
Efficacy of CAR-T immunotherapy in MET overexpressing tumors not eligible for anti-MET targeted therapy [ J Exp Clin Cancer Res, 2022, 41(1):309] PubMed: 36271379
MACC1 promotes pancreatic cancer metastasis by interacting with the EMT regulator SNAI1 [ Cell Death Dis, 2022, 13(11):923] PubMed: 36333284
STAT3 inhibition suppresses adaptive survival of ALK-rearranged lung cancer cells through transcriptional modulation of apoptosis [ NPJ Precis Oncol, 2022, 6(1):11] PubMed: 35228642
MET Oncogene Controls Invasive Growth by Coupling with NMDA Receptor [ Cancers (Basel), 2022, 14(18)4408] PubMed: 36139568
MET∆14 promotes a ligand-dependent, AKT-driven invasive growth [ Life Sci Alliance, 2022, 5(10)e202201409] PubMed: 35636967
Dysbiotic stress increases the sensitivity of the tumor vasculature to radiotherapy and c-Met inhibitors [ Angiogenesis, 2021, 10.1007/s10456-021-09771-z] PubMed: 33629198

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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