JNJ-38877618, inhibitor

JNJ-38877618

Cat. Num. AAA5755024

• Purity: 98.00%
• Synonyms: JNJ-38877618; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 5mg/mL (13.36mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C20H12F2N6
• SMILES: FC(C1=CC=C2N=CC=CC2=C1)(F)C3=NN=C4C=CC(C5=CC=NC=C5)=NN43
• CAS Number: 943540-74-7
• Target & IC50: wt Met: ic50 2nM; mutant Met: ic50 2nM
• In Vitro: JNJ-38877618 results in the 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. JNJ-38877618 causes 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. Combination treatment, are well tolerated and improved EGFR targeted therapy[1].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for JNJ-38877618, inhibitor

JNJ-38877618 is an effective and highly selective inhibitor of Met kinase (IC50s: 2 and 3nM for wild type and mutant Met, respectively).

References

Libouban M, et al. OMO-1, a potent, highly selective, orally bioavailable, Met kinase inhibitor with a favorable preclinical toxicity profile, shows both monotherapy activity, against Met pathway-driven tumors, and EGFR TKI combination activity in acquired resistance models [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 4791.
Libouban M, et al. OMO-1, a potent, highly selective, orally bioavailable, Met kinase inhibitor with a favorable preclinical toxicity profile, shows both monotherapy activity, against Met pathway-driven tumors, and EGFR TKI combination activity in acquired resistance models [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2018; 2018 Apr 14-18; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2018;78(13 Suppl):Abstract nr 4791.