化合物 FLT3/D835Y-IN-1 T61977
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
50 mg | 2648799-49-7 | ¥13,800.00 | 询底价 |
100 mg | 2648799-49-7 | ¥17,500.00 | 询底价 |
25 mg | 2648799-49-7 | ¥10,600.00 | 询底价 |
Product Introduction
Bioactivity
英文名: FLT3/D835Y-IN-1
描述: FLT3/D835Y-IN-1 (化合物13a) 是一种选择性的、口服活性的FLT3和FLT3/D835Y 抑制剂,IC50分别为 0.26 nM 和 0.18 nM。FLT3/D835Y-IN-1 具有抗癌作用,可以用于急性髓系白血病的研究。
体外活性: FLT3/D835Y-IN-1 (compound 13a) (100 nM, 3 h) potently inhibits Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells proliferation [1]. FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways [1]. Cell Proliferation Assay Cell Line: Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, and Ba/F3-FLT3-ITD-F691L cell lines, AML cells [1] Concentration: 100 nM Incubation Time: 3 h Result: Inhibited Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, MV4-11, MOLM14, and MOLM14-ITD/D835Y proliferation, with GI 50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively. Western Blot Analysis Cell Line: MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells [1]. Concentration: 3, 10, and 30 nM Incubation Time: 16 h Result: Significantly inhibited the FLT3, AKT, ERK, and STAT5 pathways at lower dosages.
体内活性: FLT3/D835Y-IN-1 (10 mg/kg, IP, daily, 6 days per week) significantly suppresses tumor growth and exhibits potent antitumor activity against MOLM14-ITD/D835Y cells [1]. FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance [1]. Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice [1]. Parameters 13a AUC last (ng*h/mL) 1360 ± 110 CL (L/h/kg) 6.96 ± 0.66 V ss (L/kg) 14.8 ± 0.7 T 1/2 (h) 1.5 ± 0.1 Animal Model: NOD/SCID mice (6 weeks, male, nine mice per group) [1] Dosage: 10 mg/kg Administration: IP, daily, 6 days per week, from day 7 to day 29 Result: Significantly suppressed tumor growth. Animal Model: ICR mice (7–8 weeks, male) [1] Dosage: 10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS) Administration: IV or Orally, single (Pharmacokinetic Analysis) Result: Displayed extremely low AUC and high clearance.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途