Parsaclisib, also known as INCB050465, is a novel PI3Kδ inhibitor which synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. INCB050465 inhibits PI3Kδ (IC50 = 1 nM at 1 mM ATP) with approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. INCB050465 demonstrates potent activity with IC50 values ranging from 0.2 to 2 nM. In addition, INCB050465 blocks the proliferation of several DLBCL and MCL cell lines in vitro (EC50 < 10 nM) and can slow tumor growth in the Pfeiffer model of DLBCL in vivo.
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名称 | Parsaclisib free base |
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Iupac 化学名称 | (4R)-4-{3-[(1S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl}pyrrolidin-2-one |
同义词 | INCB50465 HCl; INCB-50465; INCB 50465; IINCB050465; INCB-050465; INCB 050465. INCB050465 free base; Parsaclisib; Parsaclisib free base |
英文同义词 | INCB50465 HCl; INCB-50465; INCB 50465; IINCB050465; INCB-050465; INCB 050465. INCB050465 free base; Parsaclisib; Parsaclisib free base |
分子式 | C20H22ClFN6O2 |
分子量 | 432.88 |
Smile | O=C1NC[C@@H](C2=C(F)C(Cl)=CC([C@@H](N3N=C(C)C4=C(N)N=CN=C43)C)=C2OCC)C1 |
InChiKey | ZQPDJCIXJHUERQ-QWRGUYRKSA-N |
InChi | InChI=1S/C20H22ClFN6O2/c1-4-30-18-12(6-13(21)17(22)16(18)11-5-14(29)24-7-11)10(3)28-20-15(9(2)27-28)19(23)25-8-26-20/h6,8,10-11H,4-5,7H2,1-3H3,(H,24,29)(H2,23,25,26)/t10-,11-/m0/s1 |
Cas号 | 1426698-88-5 |
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