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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
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.
Targets |
c-Met (IC50 = 4 nM)
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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.
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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]
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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.
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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 |
Molecular Formula |
C19H13F2N7
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Molecular Weight |
377.35
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Exact Mass |
377.12
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Elemental Analysis |
C, 60.48; H, 3.47; F, 10.07; N, 25.98
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CAS # |
943540-75-8
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Appearance |
Solid powder
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SMILES |
CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2
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InChi Key |
JRWCBEOAFGHNNU-UHFFFAOYSA-N
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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
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Chemical Name |
6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
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Synonyms |
JNJ38877605; JNJ 38877605; JNJ-38877605
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
(2) Be sure to add the solvent(s) in order.
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 |
J Natl Cancer Inst . 2011 Apr 20;103(8):645-61 td> |