935666-88-9

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

CYT387 is an ATP-competitive small molecule JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM for JAK1 and JAK2, respectively.
CYT387 has significantly less activity against other kinases, including JAK3 (IC50=0.16 μM). CYT387 inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50 = ~1.5 μM) or Ba/F3-MPLW515L cells (IC50 = 0.2 μM), but CYT387 has considerably less activity against BCR–ABL harboring K562 cells (IC50 = 58 μM). Cell lines harboring mutated JAK2 alleles (CHRF-288-11 or Ba/F3-TEL-JAK2) were inhibited more potently than the corresponding pair harboring mutated JAK3 alleles (CMK or Ba/F3-TEL-JAK3), and STAT-5 phosphorylation was inhibited in HEL cells with an IC50 of 0.4 μM.

参考文献

[1] Pardanani A et al. Leukemia. 2009 Aug;23(8):1441-5.

[2] Tyner JW et al. Blood. 2010 Jun 24;115(25):5232-40.