Network Version
SKLB4771 Data Sheet
| Product Name: | SKLB4771 |
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| CAS No.: | 1370256-78-2 | |||||||||||
| Cat. No.: | HY-12960 | |||||||||||
| MWt: | 537.66 | |||||||||||
| Formula: | C25H27N7O3S2 | |||||||||||
| Purity : | >98% | |||||||||||
| Solubility: | DMSO : 33.33 mg/mL (61.99 mM; Need ultrasonic) | |||||||||||
| Mechanisms: | Target: Cancer | |||||||||||
| Biological Activity: | ||||||||||||
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SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue[1][2].
IC50 & Target:IC50: 10 nM (Flt3); 3.7 μM (Flt4); 1.5 μM (Aurora A); 6.8 μM (c-kit); 2.8 μM (FMS)[1]
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[1]. 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[1]. 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[1]. Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)[1]
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