JNJ-64619178 | CAS# 2086772-26-9 | PRMT5 inhibitor

MedKoo Cat#: 206820 | Name: JNJ-64619178

Description:

WARNING: This product is for research use only, not for human or veterinary use.

JNJ-64619178, also known as Onametostat, is an inhibitor of protein arginine methyltransferase 5 (PRMT5). Onametostat inhibits the growth of various cancer cells in vitro and reduces tumor growth in non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) mouse xenograft models.

Chemical Structure

JNJ-64619178

CAS#2086772-26-9

Theoretical Analysis

MedKoo Cat#: 206820

Name: JNJ-64619178

CAS#: 2086772-26-9

Chemical Formula: C22H23BrN6O2

Exact Mass: 482.1066

Molecular Weight: 483.37

Elemental Analysis: C, 54.67; H, 4.80; Br, 16.53; N, 17.39; O, 6.62

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 550.00	2 Weeks
10mg	USD 950.00	2 Weeks

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Synonym

JNJ-64619178; JNJ 64619178; JNJ64619178; Onametostat;

IUPAC/Chemical Name

(1S,2R,3S,5R)-3-(2-(2-amino-3-bromoquinolin-7-yl)ethyl)-5-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol

InChi Key

DBSMLQTUDJVICQ-CJODITQLSA-N

InChi Code

InChI=1S/C22H23BrN6O2/c23-15-8-12-3-1-11(7-16(12)28-21(15)25)2-4-13-9-17(19(31)18(13)30)29-6-5-14-20(24)26-10-27-22(14)29/h1,3,5-8,10,13,17-19,30-31H,2,4,9H2,(H2,25,28)(H2,24,26,27)/t13-,17+,18+,19-/m0/s1

SMILES Code

BrC1=C(N)N=C(C=C(CC[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C=C3)C2)C=C5)C5=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

JNJ-64619178 (Onametostat) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM.

In vitro activity:

This study found that SGC0946 (an inhibitor of DOT1L), JNJ-64619178 (an inhibitor of PRMT5) and SGC8158 (an inhibitor of PRMT7) inhibit CamA enzymatic activity in vitro at low micromolar concentrations. Reference: Epigenetics. 2022 Sep;17(9):970-981. https://pubmed.ncbi.nlm.nih.gov/34523387/

In vivo activity:

On the other hand, when the mice were treated with JNJ-64619178, the tumor growth was essentially completely inhibited. These results support that the PRMT5 inhibitor JNJ-64619178 represents a potential treatment option for CCSST. Reference: J Biol Chem. 2022 Oct;298(10):102434. https://pubmed.ncbi.nlm.nih.gov/36041632/

	Solvent	mg/mL	mM
Solubility
	DMSO	111.0	229.64

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 483.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Li BX, David LL, Davis LE, Xiao X. Protein arginine methyltransferase 5 is essential for oncogene product EWSR1-ATF1-mediated gene transcription in clear cell sarcoma. J Biol Chem. 2022 Oct;298(10):102434. doi: 10.1016/j.jbc.2022.102434. Epub 2022 Aug 27. PMID: 36041632; PMCID: PMC9513783. 2. Zhou J, Horton JR, Yu D, Ren R, Blumenthal RM, Zhang X, Cheng X. Repurposing epigenetic inhibitors to target the Clostridioides difficile-specific DNA adenine methyltransferase and sporulation regulator CamA. Epigenetics. 2022 Sep;17(9):970-981. doi: 10.1080/15592294.2021.1976910. Epub 2021 Sep 15. PMID: 34523387; PMCID: PMC9487755.

In vitro protocol:

In vivo protocol:

1. Tao, H., Yan, X., Zhu, K., et al. Discovery of novel PRMT5 inhibitors by virtual screening and biological evaluations. Chem. Pharm. Bull. (Tokyo) 67(4), 382-388 (2019). 2. Wu, T., Millar, H., Gaffney, D., et al. Abstract 4859: JNJ-64619178, a selective and pseudo-irreversible PRMT5 inhibitor with potent in vitro and in vivo activity, demonstrated in several lung cancer models. Cancer Res. 78(13_suppl.), 4859 (2018).