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JI6 (JAK3 Inhibitor VI) 是有效的,选择性的和具有口服活性的 FLT3 抑制剂。JI6抑制 FLT3-WT,FLT3-D835Y 和 FLT3-D835H 的 IC50 值分别为 ~40,8 和 4 nM。JI6 对 JAK3 和 c-Kit 也有抑制作用,IC50 值分别为 ~250 和 ~500 nM。JI6 可用于急性髓性白血病的相关研究。
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JI6 (JAK3 Inhibitor VI) 是有效的,选择性的和具有口服活性的 FLT3 抑制剂。JI6抑制 FLT3-WT,FLT3-D835Y 和 FLT3-D835H 的 IC50 值分别为 ~40,8 和 4 nM。JI6 对 JAK3 和 c-Kit 也有抑制作用,IC50 值分别为 ~250 和 ~500 nM。JI6 可用于急性髓性白血病的相关研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,130 | 现货 | |
5 mg | ¥ 2,650 | 现货 | |
10 mg | ¥ 3,970 | 现货 | |
25 mg | ¥ 6,360 | 现货 | |
50 mg | ¥ 8,690 | 现货 | |
100 mg | ¥ 11,700 | 现货 | |
500 mg | ¥ 23,500 | 现货 |
产品描述 | JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia. |
体外活性 | JI6 (3-1000 nM; 1-4 days) inhibits MV4-11 cell viability in a dose-dependent manner with IC50 of ∼25 nM. JI6 (1-2000 nM; 48 h) potently inhibits the viability of HCD-57 cells expressing FLT3-ITD, FLT3-D835Y and FLT3-D835H with IC50 of ∼40 nM. JI6 has no effect on the parent HCD-57 or JAK2V617F expressing cells. JI6 (100-500 nM; 24 h) induce apoptosis and cell cycle arrest in HCD-57 cells expressing FLT3-ITD and FLT3-D835Y. JI6 (50-500 nM; 3 h) inhibits phosphorylation of FLT3, ERK and Akt in HCD-57 cells expressing FLT3-ITD and FLT3-D835Y[1]. |
体内活性 | JI6 (15 mg/kg; i.p. daily for 3 weeks) inhibits the proliferation of HCD-57 expressing FLT3-D835Y in SCID mouse and prolong the survival. JI6 (25 mg/kg; p.o. daily for 3 weeks) inhibits myeloproliferative phenotype in FLT3-ITD knock-in mice. JI6 (100 mg/kg; a single i.p.) significantly inhibits FLT3 phosphorylation and downstream signal transduction in mice expressing FLT3-D835Y[1]. |
别名 | JAK3 Inhibitor VI |
分子量 | 383.42 |
分子式 | C19H17N3O4S |
CAS No. | 856436-16-3 |
Smiles | CS(=O)(O)=O.O=C(/C1=C\C2=CC=CN2)NC(C=C3)=C1C=C3C4=CN=CC=C4 |
密度 | no data available |
存储 | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 4.5 mg/mL (11.7 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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