For research use only. Not for therapeutic Use.
NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex[1].
| Catalog Number | I041287 |
| CAS Number | 2416130-57-7 |
| Synonyms | 3-[4-[1-[[(3S)-1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]pyrrolidin-3-yl]methyl]piperidin-4-yl]anilino]-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide |
| Molecular Formula | C43H51N11O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C43H51N11O6/c1-49-19-20-53(43(49)60)31-3-2-15-52(25-31)35-22-45-37(38(44)56)39(47-35)46-29-6-4-27(5-7-29)28-13-16-50(17-14-28)23-26-12-18-51(24-26)30-8-9-32-33(21-30)42(59)54(41(32)58)34-10-11-36(55)48-40(34)57/h4-9,21-22,26,28,31,34H,2-3,10-20,23-25H2,1H3,(H2,44,56)(H,46,47)(H,48,55,57)/t26-,31+,34?/m0/s1 |
| InChIKey | WFDYOAWNEOGIPM-NJZOVTIDSA-N |
| SMILES | CN1CCN(C1=O)C2CCCN(C2)C3=CN=C(C(=N3)NC4=CC=C(C=C4)C5CCN(CC5)CC6CCN(C6)C7=CC8=C(C=C7)C(=O)N(C8=O)C9CCC(=O)NC9=O)C(=O)N |
| Reference | [1]. Zhang D, et al. NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts. Blood. 2023 Mar 30;141(13):1584-1596. |
