Description
JNJ-64619178 is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.
Product information
CAS Number: 2086772-26-9
Molecular Weight: 483.36
Formula: C22H23BrN6O2
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
Smiles: NC1N=CN=C2C=1C=CN2[C@@H]1C[C@H](CCC2C=CC3=CC(Br)=C(N)N=C3C=2)[C@@H](O)[C@H]1O
InChiKey: DBSMLQTUDJVICQ-CJODITQLSA-N
InChi: 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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (258.61 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
JNJ-64619178 binds simultaneously to the S-adenosylmethionine (SAM)- and protein substrate- binding pockets of the PRMT5/MEP50 complex with a pseudo-irreversible mode-of-action. JNJ-64619178 shows potent and broad inhibition of cellular growth.
In Vivo:
Oral administration of JNJ-64619178 results in efficient inhibition of dimethylation of SMD1/3 proteins, components of the splicing machinery and direct substrates of the methylosome, in several non-small cell lung cancer and small cell lung cancer cancer mouse xenograft models.
Products are for research use only. Not for human use.
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