Onametostat (JNJ-64619178)

Catalog No.S8624

For research use only.

Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.

Onametostat (JNJ-64619178) Chemical Structure

CAS No. 2086772-26-9

Selleck's Onametostat (JNJ-64619178) has been cited by 2 Publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.
Targets
PRMT5 [1]
0.14 nM
In vitro

JNJ-64619178 binds into the SAM binding pocket and reaches the substrate binding pocket to inhibit PRMT5/MEP50 function in a time-dependent manner. Broad cell line panel profiling of JNJ-64619178 reveals a wide range of sensitivity, which is indicative of a genomic dependency instead of a general cytotoxic on-target consequence of PRMT5 inhibition[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Ml;4SpVv[3Srb36gZZN{[Xl? MW\Jcohq[mm2aX;uJI9nKG[3bHytcIVv\3SqIHj1cYFvKE5vdHXycYlv[WxiRlzBS{11[WepZXSgVHJOXDVxZoXscEBt\W6pdHigUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCPRWC1NEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCVLXHk[Y5we3muLVytbI9ud2O7c4TlbY5mKG[xcn3heIlwdiC3c3nu[{BpfW2jbjDy[YNwdWKrbnHueEAtKEmFNUC9NE4xODBzM988US=> NVjjRYFFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVYxOTFpPkOwPVU3ODFzPD;hQi=>
Sf9 MX3GeY5kfGmxbjDhd5NigQ>? M4nuV|EzOCCvaX7z NWfBU5ZWUW6qaXLpeIlwdiCxZjDmeYxtNWynbnf0bEBpfW2jbjDOMZRmem2rbnHsJGZNSUdvdHHn[4VlKFCUTWS1JIV5eHKnc4Pl[EBqdiCVZkmgbY5{\WO2IHPlcIx{KHW|aX7nJIhqe3SxbnWgTFJCKGG|IIDldJRq\GViYX\0[ZIhOTJyIH3pcpMhcW5icILld4Vv[2Vib3[gV2FOKGK7IHjp[4ghfGi{b4XnbJB2fCCvYYPzJJNx\WO2cn;t[ZRmeiCjc4PhfUwhUUN3ME2wMlAxODF2zszN M2PsWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5|MEO2OlYyPzxxYU6=
A549 MnLxSpVv[3Srb36gZZN{[Xl? Mof6OFghcHK| NX;BcGtQUW6qaXLpeIlwdiCxZjDQVm1VPSCrbjDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC|RF3BJJBzd2S3Y4Tpc44h[W[2ZYKgOFghcHK|IHL5JGhw\WOqc4SgV5RicW5xSFPTJGNmdGyPYYPrJGRm\XBiUnXkJHN1[WmwIHLhd4VlKGmvbYXuc4hqe3SxY3jlcYl{fHK7IH3leIhw\CxiSVO1NF0xNjByMEK1{txO NWjCUolpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVYxOTFpPkOwPVU3ODFzPD;hQi=>
HEK293 M3XGc2Z2dmO2aX;uJIF{e2G7 NVjldpBWPjBibXnudy=> MmDjTY5pcWKrdHnvckBw\iCqdX3hckBPNXSncn3pcoFtKE[OQVeteIFo\2WmIGDSUXQ2KCh{IITvJIVv\CliZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyC3c3nu[{BjcW:2aX75cIF1\WRiSELBJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkA3OCCvaX7zJIlvKHC{ZYPlcoNmKG:oIGPBUUBjgSCqaXfoJJRpem:3Z3jweZQhdWG|czDzdIVkfHKxbXX0[ZIh[XO|YYmsJGlEPTB;MD6wNFY{|ryP MlXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6N{CyOVgoRjJ7OEewNlU5RC:jPh?=
In vivo JNJ-64619178, dosed orally (10 mg/kg, every day), shows selective and efficient blockage of the methylation of SMD1/3 proteins, which are crucial components of the spliceosome and substrates of PRMT5/MEP50. JNJ-64619178 also demonstrates tumor regression in a biomarker-driven human small cell lung cancer xenograft model (NCI-H1048) and prolongs tumor growth inhibition after dosing cessation. In rodent and nonrodent toxicology studies, a tolerated dose of JNJ-64619178 has been identified, with the observed toxicity consistent with on-target activity. In summary, JNJ-64619178 has a favorable preclinical package that supports clinical testing in patients diagnosed with lung cancer and hematologic malignancies1[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 483.36
Formula

C22H23BrN6O2

CAS No. 2086772-26-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C(C(C(C1N2C=CC3=C(N=CN=C32)N)O)O)CCC4=CC5=NC(=C(C=C5C=C4)Br)N

In vivo Formulation Calculator (Clear solution)

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03573310 Active not recruiting Drug: JNJ-64619178 Neoplasms|Solid Tumor Adult|Non-Hodgkin Lymphoma|Myelodysplastic Syndromes Janssen Research & Development LLC July 13 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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