Momelotinib|1056634-68-4|(CYT387)-陌孚医药/Medlife

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Momelotinib (Synonyms: CYT387)

目录号: PL14920 纯度: ≥98%

CAS No. :1056634-68-4

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中文名称	Momelotinib
中文别名	3-[(氨基羰基)氨基]-5-(3-氟苯基)-N-(3S)-3-哌啶基-2-噻吩羧胺;N-(氰基甲基)-4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯甲酰胺;MOMELO锡IB;N-(氰基甲基)-4-【2-【【4-(4-吗啉基)苯基】氨基】-4-嘧啶基】苯基酰胺;N-(氰基甲基)-4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯甲酰胺(CYT387)
英文名称	Momelotinib
英文别名	N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide;CYT387;CYT-387;Momelotinib (CYT387);momelotinib（CYT-387）;N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)-amino)pyrimidin-4-yl)benzamide;N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]Benzamide;momelotinib;CYT 11387;LM-1149;Orange solid;CYT 387(CYT 11387);CYT387(momelotinib);momelotinib(JAK inhibitor)ORPHAN DRUG;CYT 387;N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide;6O01GMS00P;AK102858;N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide;N-(cyanomethyl)-4-(2-{[4-(morpholin-4-yl)phenyl]amino}pyrimidin-4-yl)be;Momelotinib
Cas No.	1056634-68-4
分子式	C₂₃H₂₂N₆O₂
分子量	414.46
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Momelotinib (CYT387) 是 ATP 竞争性的 JAK1/JAK2 抑制剂，IC₅₀ 值分别为 11 nM/18 nM，是对 JAK3 选择性的 10 倍左右。

生物活性

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC 50 a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

性状

Solid

IC50 & Target[1][2]

JAK1 11 nM (IC50) JAK2 18 nM (IC50

体外研究(In Vitro)

Momelotinib (CYT387) inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, Momelotinib (CYT387) also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, Momelotinib (CYT387) has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2 μM-4 μM. Momelotinib (CYT387) inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib (CYT387) induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies PS-341 and L-PAM in primary multiple myeloma (MM) cells.

体内研究(In Vivo)

In a murine MPN model, Momelotinib (CYT387) normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445.
[2]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899.

溶解度数据	In Vitro: DMSO : 20.83 mg/mL (50.26 mM; ultrasonic and warming and heat to 80°C)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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