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Purity: ≥98%
OMO-1 (formerly known as JNJ-38877618) is a novel, potent, highly selective and orally bioavailable Met kinase inhibitor with nM binding affinity (Kd=1.4 nM) and enzyme inhibitory activity against wt and M1268T mutant MET (IC50 2 and 3 nM ). Proliferation, colony formation, and motility assays were used to evaluate the inhibitory effects of MET. Against MET Ampl/mutant and therapy-resistant models, OMO-1 demonstrated nM potency. In three models (the SNU5 MET amp gastric, the U87-MG HGF autocrine glioblastoma, and the Hs746T MET exon 14 skipping mutant gastric cancer) OMO-1 completely inhibited the growth of the tumors in vivo. OMO-1 caused MET kinase activation to be inhibited in a dose- and time-dependent manner, leading to the regression of large MET amplified EBC-1 SqNSCLC. The target shut down duration was significantly longer than the plasma exposure times. The well-tolerated combination treatments enhanced the EGFR-targeted therapy. OMO-1 as a single agent had no effect on NSCLC HCC827 EGFR; however, when combined with erlotinib, the onset of tumor recurrence was delayed. It was discovered that the obtained EGFR inhibitor resistant model HCC827-ER1 was MET amplified. In this model, erlotinib and OMO-1 individually inhibited tumor growth, but together they caused tumor regression. OMO-1, a single agent, caused tumor stasis in a PDX resistant to EGFR inhibitors with MET amplification, while MetMab/erlotinib only delayed the growth of the tumor. The strong preclinical activity seen is in favor of OMO-1's continued clinical development in individuals with tumors driven by the MET pathway. with 2 and 3 nM IC50s for mutant and wild type Met, respectively.
| Targets |
wt Met (IC50 = 2 nM); mutant Met (IC50 = 2 nM)
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|---|---|
| ln Vitro |
OMO-1 (formerly JNJ-38877618) is an oral bioavailable, highly selective, potent Met kinase inhibitor with nM binding affinity (Kd=1.4 nM) and IC50 values of 2 and 3 nM for both wild-type and M1268T mutant Met. Assays for colony formation, motility, and proliferation are used to evaluate the effects of met inhibitors. When it comes to Met Ampl/mutant and therapy-resistant models, JNJ-38877618 exhibits nM potency[1].
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| ln Vivo |
JNJ-38877618 causes total inhibition of tumor growth in three models: Hs746T Met exon 14 skipping mutant gastric cancer, U87-MG HGF autocrine glioblastoma, and SNU5 Met amp gastric cancer. Large Met amplified EBC-1 SqNSCLC is regressed when exposed to JNJ-38877618, which inhibits Met kinase activation in a time- and dose-dependent manner. The duration of target shut down is significantly longer than that of plasma exposure times. Combination therapies have enhanced EGFR targeted therapy and are well tolerated[1].
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| References |
| Molecular Formula |
C20H12F2N6
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|---|---|
| Molecular Weight |
374.346289634705
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| Exact Mass |
374.11
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| Elemental Analysis |
C, 64.17; H, 3.23; F, 10.15; N, 22.45
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| CAS # |
943540-74-7
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| Related CAS # |
943540-74-7
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| Appearance |
Solid powder
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| SMILES |
C1=CC2=C(C=CC(=C2)C(C3=NN=C4N3N=C(C=C4)C5=CC=NC=C5)(F)F)N=C1
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| InChi Key |
KOAWAWHSMVKCON-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H12F2N6/c21-20(22,15-3-4-16-14(12-15)2-1-9-24-16)19-26-25-18-6-5-17(27-28(18)19)13-7-10-23-11-8-13/h1-12H
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| Chemical Name |
6-[difluoro-(6-pyridin-4-yl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]quinoline
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| Synonyms |
JNJ-38877618; JNJ 38877618; JNJ38877618
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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) |
DMSO: 5~10 mg/mL (13.4~26.7 mM)
Ethanol: ~2 mg/mL (~5.3 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*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 |
| NCT01964872 | Completed | Drug: JNJ-38877618: Part 1a Drug: JNJ-38877618: Part 1b |
Healthy Volunteers | Janssen Cilag N.V./S.A. | November 2013 | Phase 1 |
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