JNJ-38877605

Alias: JNJ38877605; JNJ 38877605; JNJ-38877605
Cat No.:V0601 Purity: ≥98%
JNJ-38877605 (JNJ38877605) is an orally bioavailable small-moleculeinhibitor of c-Met with potential antitumor activity.
JNJ-38877605 Chemical Structure CAS No.: 943540-75-8
Product category: c-MET
This product is for research use only, not for human use. We do not sell to patients.
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25mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

JNJ-38877605 (JNJ38877605) is an orally bioavailable small-molecule inhibitor of c-Met with potential antitumor activity. It exhibits 600-fold selectivity for inhibiting c-Met over 200 other kinases and inhibits it with an IC50 of 4 nM.

Biological Activity I Assay Protocols (From Reference)
Targets
c-Met (IC50 = 4 nM)
ln Vitro
JNJ-38877605 potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro and exhibits more than 600-fold selectivity for c-Met when compared to more than 200 other diverse tyrosine and serine-threonine kinases.[1] One important factor in invasive growth that is significantly reduced in EBC1, GTL16, NCI-H1993, and MKN45 cells is JNJ-38877605 (500 nM) phosphorylation of Met and RON.[2] uPAR, IL-6, GROa, and IL-8 secretion in GTL16 cells are all modulated by JNJ-38877605, according to a recent study.
ln Vivo
JNJ-38877605, when administered orally at 40 mg/kg/day for 72 hours in mice with established GTL16 xenografts, causes a statistically significant reduction in human IL-8 plasma levels (from 0.150 ng/mL to 0.050 ng/mL) and GROα plasma levels (from 0.080 ng/mL to 0.030 ng/mL). At the same dosage, however, blood levels of uPAR drop to levels greater than 50%.[3]
Enzyme Assay
JNJ-38877605 is an ATP-competitive inhibitor of c-Met with an IC50 of 4 nM that is 600 times more selective for c-Met than 200 other tyrosine and serine-threonine substrates.
Animal Protocol
GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
≤40 mg/kg/day
Administered via p.o.
References

[1]. JNJ-38877605: a selective Met kinase inhibitor inducing regression of Met-driven tumor models.

[2]. J Natl Cancer Inst . 2011 Apr 20;103(8):645-61.

[3]. Int J Cancer . 2012 Mar 15;130(6):1357-66.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H13F2N7
Molecular Weight
377.35
Exact Mass
377.12
Elemental Analysis
C, 60.48; H, 3.47; F, 10.07; N, 25.98
CAS #
943540-75-8
Appearance
Solid powder
SMILES
CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2
InChi Key
JRWCBEOAFGHNNU-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H13F2N7/c1-27-11-13(10-23-27)16-6-7-17-24-25-18(28(17)26-16)19(20,21)14-4-5-15-12(9-14)3-2-8-22-15/h2-11H,1H3
Chemical Name
6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
Synonyms
JNJ38877605; JNJ 38877605; JNJ-38877605
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~37 mg/mL (~98.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6501 mL 13.2503 mL 26.5006 mL
5 mM 0.5300 mL 2.6501 mL 5.3001 mL
10 mM 0.2650 mL 1.3250 mL 2.6501 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00651365 Terminated Drug: JNJ-38877605 Neoplasms Johnson & Johnson Pharmaceutical
Research & Development, L.L.C.
February 2008 Phase 1
Biological Data
  • J Natl Cancer Inst . 2011 Apr 20;103(8):645-61
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