1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. JNJ-38877618

JNJ-38877618 

Cat. No.: HY-111050 Purity: 99.01%
Handling Instructions

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.

For research use only. We do not sell to patients.

JNJ-38877618 Chemical Structure

JNJ-38877618 Chemical Structure

CAS No. : 943540-74-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 231 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 310 In-stock
Estimated Time of Arrival: December 31
50 mg USD 910 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Technical Information

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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.

IC50 & 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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (13.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6713 mL 13.3565 mL 26.7130 mL
5 mM 0.5343 mL 2.6713 mL 5.3426 mL
10 mM 0.2671 mL 1.3356 mL 2.6713 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.5 mg/mL (1.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (1.34 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.5 mg/mL (1.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

374.35

Formula

C₂₀H₁₂F₂N₆

CAS No.

943540-74-7

SMILES

FC(C1=CC=C2N=CC=CC2=C1)(F)C3=NN=C4C=CC(C5=CC=NC=C5)=NN43

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
JNJ-38877618
Cat. No.:
HY-111050
Quantity:

JNJ-38877618

Cat. No.: HY-111050