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 ¦ÌM). CYT387 inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50 = ~1.5 ¦ÌM) or Ba/F3-MPLW515L cells (IC50 = 0.2 ¦ÌM), but CYT387 has considerably less activity against BCR¨CABL harboring K562 cells (IC50 = 58 ¦ÌM). 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 ¦ÌM

June 21, 2017

prudect name : 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 ¦ÌM). CYT387 inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50 = ~1.5 ¦ÌM) or Ba/F3-MPLW515L cells (IC50 = 0.2 ¦ÌM), but CYT387 has considerably less activity against BCR¨CABL harboring K562 cells (IC50 = 58 ¦ÌM). 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 ¦ÌM
Cyt387

Synonyms: CYT11387CAS NO: 1056634-68-4Molecular Formula: C23H22N6O2Molecular Weight: 414.46Purity: 98% minSolubility: In DMSOStorage: -20¡æ


ARQ197 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18509186