CYT387 sulfate salt,1056636-06-6

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YZ剂描述：

产品名称：CYT387 sulfate salt

产品别名：N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide, sulfuric acid

英文别名：CYT-387 sulfate;CYT 387 sulfate;momelotinib sulfate

靶点：JAK

CAS：1056636-06-6

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

CYT387 sulfate salt is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3.

溶解性：DMSO: ≥ 6.1 mg/mL

体外研究：

Momelotinib sulfate (CYT387 sulfate salt) inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC₅₀=1.5 μM) or Ba/F3-MPLW515L cells (IC₅₀=200 nM), but has considerably less activity against BCR-ABL harboring K562 cells (IC₅₀=58 μM) and FLT3 mutation harboring MV4-11 cells (IC₅₀=3 μM). Proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 is inhibited with an IC₅₀ value of 1.4 μM, consistent with the established role of IL-3-dependent signaling in the parental cell line.

体内研究：

Momelotinib sulfate (CYT387 sulfate salt) at twice the dose used in disease model (50 and 100 mg/kg) has little to no effect on peripheral blood counts over a period of 8 weeks. Median plasma peak concentrations are 7.1 μM with the lower dose and 32.1μM with the higher dose, with a half-life of approximately 2 hours. Trough levels at 12 hours are 10nM for the 25 mg/kg and 900nM for the 50 mg/kg dose. At day 34 after transplantation, the mean white blood cell counts and hematocrit values of the entire cohort exceeded the normal range for Balb/c mice by more than 1 SD. At this point, 6 mice are sacrificed and subjected to autopsy. In the remaining animals, treatment is initiated with 25 mg/kg Momelotinib sulfate (CYT387 sulfate salt), 50 mg/kg Momelotinib sulfate (CYT387 sulfate salt), or vehicle, administered twice daily by oral gavage (12 mice per treatment group). A rapid drop of the white cell counts is apparent in both dose cohorts as early as 6 days after initiation of treatment and a decline of the hematocrit is apparent after 20 days. After oral dosing, Momelotinib sulfate (CYT387 sulfate salt) exhibits high plasma concentrations (C_max= 40.4 μM; T_max=4 h), with quantitative absolute oral bioavailability and an apparent half life of 2.4 h. The high oral bioavailability, can likely be partly ascribed to the low blood clearance of Momelotinib sulfate (CYT387 sulfate salt) (6.3 mL/min/kg) and therefore low susceptibility to hepatic first pass metabolism.

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