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943540-74-7

943540-74-7 Structure

943540-74-7 Structure
IdentificationBack Directory
[Name]

JNJ-38877605
[CAS]

943540-74-7
[Synonyms]

OMO-1)
JNJ-38877618
JNJ-38877618 (OMO1
6-[Difluoro[6-(4-pyridinyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
6-(difluoro(6-(pyridin-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline
Quinoline, 6-[difluoro[6-(4-pyridinyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]-
[Molecular Formula]

C20H12F2N6
[MDL Number]

MFCD31657377
[MOL File]

943540-74-7.mol
[Molecular Weight]

374.35
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 5 mg/mL (13.36 mM)
[form ]

Solid
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

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.
[Biological Activity]

JNJ-38877618 (OMO-1) is a potent, highly selective, and orally bioavailable Met (c-Met) kinase inhibitor with a Kd of 1.4 nM. Its IC50 values for wild-type Met (c-Met) and mutant Met (c-Met) (M1268T) were 2 nM and 3 nM, respectively.
[in vivo]

In vivo, JNJ-38877618(OMO-1) completely inhibited tumor growth in 3 tumor models: SNU5 MET amp gastric cancer model, U87-MG HGF autocrine glioblastoma model, and exon 14 skipping deletion mutation Hs746T gastric cancer model of MET gene. Administration of OMO-1 in combination with other drugs is well tolerated and can improve and enhance the effect of EGFR-targeted therapy. Although single-agent OMO-1 has no effect on NSCLC HCC827 EGFR, its combination with erlotinib can delay tumor recurrence.

[target]

< /table>
TargetValue
Met
(Cell-free assay)
2 nM
MET (M1268T)
(Cell-free assay)
3 nM
[storage]

Store at -20°C
[References]

[1] 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 acquire
Spectrum DetailBack Directory
[Spectrum Detail]

JNJ-38877605(943540-74-7)1HNMR
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