JI6
作者：齊岳
發(fā)布時(shí)間：2023-08-22
09:22:15
點(diǎn)擊數(shù)：
產(chǎn)品名稱：JI6
產(chǎn)品描述：
| 產(chǎn)品描述 | JI6 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. |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 別名 | JAK3 Inhibitor VI |
| 分子量 | 383.42 |
| 分子式 | C19H17N3O4S |
| CAS No. | 856436-16-3 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 4.5 mg/mL (11.7 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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