Momelotinib
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:05:26
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：Momelotinib
產(chǎn)品描述：
| 產(chǎn)品描述 | Momelotinib is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. |
| 靶點(diǎn)活性 | JAK1:11 nM, JAK2:18 nM |
| 體外活性 | 作用于鼠MPN 模型時(shí),CYT387可使血球密度,白細(xì)胞數(shù)和脾臟大小正?；?并恢復(fù)炎性細(xì)胞因子生理水平. |
| 體內(nèi)活性 | 在體外,CYT387對(duì)IL-3刺激的親本Ba/F3細(xì)胞增殖有抑制作用（IC50：1400 nM）。此外,CYT387對(duì)體外JAK2V617F陽(yáng)性PV患者紅系集落生長(zhǎng)的抑制效果與之相似（IC50：2-4 μM）。CYT387抑制IGF-1和IL-6誘導(dǎo)的Ras/MAPK和PI3K/AKT信號(hào)。且在原發(fā)性多發(fā)骨髓瘤細(xì)胞中,CYT387 單獨(dú)使用,或與MM**藥硼替佐米和美法侖聯(lián)用可誘發(fā)細(xì)胞凋亡。CYT387對(duì)JAK1和JAK2（IC50：11 nM和18 nM）的選擇性比JAK3激酶(IC50為155 nM)高9倍。CYT387還可作用于組成型激活的 JAK2 或 MPL信號(hào) 的細(xì)胞系,包括 Ba/F3-MPLW515L細(xì)胞（IC50：200 nM）,CHRF-288-11細(xì)胞（IC50：1 nM）和Ba/F3-TEL-JAK2細(xì)胞（IC50：700 nM）,還抑制細(xì)胞增殖。 |
| 激酶實(shí)驗(yàn) | Cell-free kinase activity assays: Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument. |
| 細(xì)胞實(shí)驗(yàn) | Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37 °C with 5% CO2</sub(Only for Reference) |
| 別名 | CYT11387, CYT387, LM-1149 |
| 分子量 | 414.46 |
| 分子式 | C23H22N6O2 |
| CAS No. | 1056634-68-4 |
存儲(chǔ)
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 69 mg/mL (166.5 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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