Onametostat (JNJ-64619178)

For research use only.

Catalog No.S8624

1 publication

Onametostat (JNJ-64619178) Chemical Structure

CAS No. 2086772-26-9

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.

Selleck's Onametostat (JNJ-64619178) has been cited by 1 publication

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 NU\Ibo1QTnWwY4Tpc44h[XO|YYm= MYfJcohq[mm2aX;uJI9nKG[3bHytcIVv\3SqIHj1cYFvKE5vdHXycYlv[WxiRlzBS{11[WepZXSgVHJOXDVxZoXscEBt\W6pdHigUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCPRWC1NEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCVLXHk[Y5we3muLVytbI9ud2O7c4TlbY5mKG[xcn3heIlwdiC3c3nu[{BpfW2jbjDy[YNwdWKrbnHueEAtKEmFNUC9NE4xODBzM988US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3NkCxNUc,OzB7NU[wNVE9N2F-
Sf9 MVfGeY5kfGmxbjDhd5NigQ>? NXLUem04OTJyIH3pcpM> MmexTY5pcWKrdHnvckBw\iCodXzsMYxmdme2aDDoeY1idiCQLYTldo1qdmGuIF\MRWcufGGpZ3XkJHBTVVR3IHX4dJJme3OnZDDpckBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHjpd5RwdmViSELBJIF{KHCncITp[IUh[W[2ZYKgNVIxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiU1HNJIJ6KGirZ3igeIhzd3WpaID1eEBu[XO|IIPw[YN1em:vZYTldkBie3OjeTygTWM2OD1yLkCwNFE1|ryP MmfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|Nk[2NVcoRjNyM{[2OlE4RC:jPh?=
A549 M37ER2Z2dmO2aX;uJIF{e2G7 NGTrc5k1QCCqcoO= M1vkSWlvcGmkaYTpc44hd2ZiUGLNWFUhcW5iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4he0SPQTDwdo9lfWO2aX;uJIFnfGW{IES4JIhzeyCkeTDIc4VkcHO2IGP0ZYlvN0iFUzDD[YxtVWG|azDE[YVxKFKnZDDTeIFqdiCkYYPl[EBqdW23bn;obZN1d2OqZX3pd5RzgSCvZYToc4QtKEmFNUC9NE4xODB{Nd88US=> NFfEemo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1OlAyOSd-M{C5OVYxOTF:L3G+
HEK293 M1K4NGZ2dmO2aX;uJIF{e2G7 MnLCOlAhdWmwcx?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJG4ufGW{bXnuZYwhTkyDRz30ZYdo\WRiUGLNWFUhMDJidH:g[Y5lMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KHW|aX7nJIJqd3SrbonsZZRm\CCKMlGgZZMhe3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFYxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiU1HNJIJ6KGirZ3igeIhzd3WpaID1eEBu[XO|IIPw[YN1em:vZYTldkBie3OjeTygTWM2OD1yLkCwOlPPxE1? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh5MEK1PEc,Ojl6N{CyOVg9N2F-

... Click to View More Cell Line Experimental Data

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (206.88 mM)
Ethanol '-1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 483.36
Formula

C22H23BrN6O2

CAS No. 2086772-26-9
Storage powder
in solvent
Synonyms N/A
Smiles C1C(C(C(C1N2C=CC3=C(N=CN=C32)N)O)O)CCC4=CC5=NC(=C(C=C5C=C4)Br)N

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID