Momelotinib sulfate CYT387 sulfate salt|cas:1056636-06-6|西域试剂

Momelotinib sulfate CYT387 sulfate salt,98.04%

产品编号：Bellancom-10962| CAS NO：1056636-06-6| 分子式：C₂₃H₂₆N₆O₁₀S₂| 分子量：610.62

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货号	价格	库存与货期
Bellancom-10962	￥850.00	杭州北京（现货）
Bellancom-10962	￥1252.00	杭州北京（现货）
Bellancom-10962	￥3464.00	杭州北京（现货）
Bellancom-10962	￥5388.00	杭州北京（现货）

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Momelotinib sulfate CYT387 sulfate salt

产品介绍

Momelotinib sulfate (CYT387 sulfate salt) 是一种 ATP竞争性的 JAK1/JAK2 抑制剂，IC₅₀ 分别为 11 nM/18 nM，作用于JAK3时，IC₅₀ 为 155 nM。

生物活性

Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC₅₀=155 nM).

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 220 mg/mL (360.29 mM; Need ultrasonic)

H₂O : 100 mg/mL (163.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6377 mL	8.1884 mL	16.3768 mL
5 mM	0.3275 mL	1.6377 mL	3.2754 mL
10 mM	0.1638 mL	0.8188 mL	1.6377 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (163.77 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5.5 mg/mL (9.01 mM); Clear solution

此方案可获得 ≥ 5.5 mg/mL (9.01 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5.5 mg/mL (9.01 mM); Clear solution

此方案可获得 ≥ 5.5 mg/mL (9.01 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5.5 mg/mL (9.01 mM); Clear solution

此方案可获得 ≥ 5.5 mg/mL (9.01 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。