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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
FLT3-IN-1
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- 规格:
10 mM * 1 mL/1 mg/2 mg/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1952.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥776.0 |
| 规格: | 2 mg | 产品价格: | ¥1100.0 |
| 规格: | 5 mg | 产品价格: | ¥1650.0 |
| 规格: | 10 mg | 产品价格: | ¥2475.0 |
| 规格: | 25 mg | 产品价格: | ¥4200.0 |
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SKLB4771
CAS No. : 1370256-78-2
MCE 国际站:SKLB4771
产品活性:SKLB4771 是一种高效的 Flt3 抑制剂,IC50 为 10 nM。SKLB4771 能够下调 FLT3/STAT5/ERK 磷酸化水平,阻断细胞增殖,并诱导肿瘤组织中的细胞凋亡 (apoptosis)。
研究领域:Protein Tyrosine Kinase/RTK | Apoptosis
In Vitro: SKLB4771 (compound 20c) (72 h) inhibits FLT3-ITD-expressing MV4-11 cells with an IC50 value of 6 nM, and inhibits other cancer cells with IC50s of 3.05 μM (Jurkat), 6.25 μM (Ramos), 3.72 μM (PC-9), 6.94 μM (H292), and 8.91 μM (A431), respectively.
SKLB4771 (0-300 nM; 20 h) inhibits FLT3 phosphorylation and also decreases the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 at concentrations >0.1 μM.
In Vivo: SKLB4771 (20-100 mg/kg; i.p.; once daily; 21 d) inhibits tumor growth in vivo without significant weight loss or any other obvious signs of toxicity on mice.
Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)
| Cmax (μg/mL) | T1/2 (h) | AUCmax (h·μg/mL) | Tmax (h) | CLobs (L/h/kg) |
| 5.31 | 13.9 | 21.86 | 1.0 | 2.21 |
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