WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206820
CAS#: 2086772-26-9
Description: Onametostat, also known as JNJ-64619178, is an inhibitor of protein arginine methyltransferase 5 (PRMT5). It 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.
MedKoo Cat#: 206820
Name: Onametostat
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
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
| 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 | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 111.0 | 229.64 |
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: | 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 vivo 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. |
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).
