943540-74-7
943540-74-7 structure
- Name: JNJ-38877618
- Chemical Name: JNJ-38877618
- CAS Number: 943540-74-7
- Molecular Formula: C20H12F2N6
- Molecular Weight: 374.35
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Met/HGFR
- Create Date: 2018-08-10 09:58:31
- Modify Date: 2024-01-02 10:44:28
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JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
| Name | JNJ-38877618 |
|---|
| Description | JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively. |
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| Related Catalog | |
| Target |
IC50: 2 nM (wt Met), 2 nM (mutant Met)[1] |
| In Vitro | OMO-1 (formerly JNJ-38877618), is a potent, highly selective, orally bioavailable Met kinase inhibitor with nM binding affinity (Kd=1.4 nM) and enzyme inhibitory activity against wt and M1268T mutant Met (2 and 3 nM IC50). Met inhibitory effects are assessed in proliferation, colony formation and motility assays. JNJ-38877618 displays nM potency against Met Ampl/mutant and therapy resistant models[1]. |
| In Vivo | JNJ-38877618 induces complete inhibition of tumor growth in 3 models: the SNU5 Met amp gastric, U87-MG HGF autocrine glioblastoma and Hs746T Met exon 14 skipping mutant gastric cancer. JNJ-38877618 induces regression of large Met amplified EBC-1 SqNSCLC where JNJ-38877618 leads to dose- and time-dependent inhibition of Met kinase activation, with the duration of target shut down considerably exceeding plasma exposure times. Combination treatments are well tolerated and improved EGFR targeted therapy[1]. |
| References |
| Molecular Formula | C20H12F2N6 |
|---|---|
| Molecular Weight | 374.35 |
| Storage condition | 2-8℃ |