SKLB4771
CAS No. : 1370256-78-2
(Synonyms: FLT3-IN-1)
| Size | Price | Stock |
|---|---|---|
| 2mg | $110 | In-stock |
| 5mg | $165 | In-stock |
| 10mg | $250 | In-stock |
| 25mg | $500 | In-stock |
| 50mg | $800 | In-stock |
| 100mg | $1200 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-12960 |
| M.Wt: | 537.66 |
| Formula: | C25H27N7O3S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 33.33 mg/mL (ultrasonic) |
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]
| 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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