JNJ-38877618 free base · Synonyms: JNJ 38877618 · JNJ38877618

JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor.

For research use only. Not for human or veterinary use.

Target c-Met/HGFR

Research area Cancer

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Data Sheet SDS COA

JNJ-38877618 structure

CAS No.: 943540-74-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 598.00	BP-02371-250mg	In stock	Get quote
500 mg	USD 1,050.00	BP-02371-500mg	In stock	Get quote
1 g	USD 1,690.00	BP-02371-1g	In stock	Get quote
5 g	Inquire	BP-02371-5g	In stock	Inquire

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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.

Biological activity

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 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

Identifiers

SMILES: C1=CC2=C(C=CC(=C2)C(C3=NN=C4N3N=C(C=C4)C5=CC=NC=C5)(F)F)N=C1
InChIKey: KOAWAWHSMVKCON-UHFFFAOYSA-N

Specifications

MW (average): 374.3463
Formula: C₂₀H₁₂F₂N₆
CAS No.: 943540-74-7
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Pure form 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 5 mg/mL

Documents

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

Same target

Search c-Met/HGFR

Same research area

Search Cancer