FLT3-IN-1

Research use only, not for human use.

FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.

FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.

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 Western Blot Analysis Cell Line:MV4-11 cells Concentration:0, 30, 100, 300 nM Incubation Time:20 hours Result:Resulted inhibition against the human FLT3 kinase in a dose-dependent manner, and decreased the phosphorylation level of STAT5 and ERK1/2 at 100 nM and 300 nM.

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.)Animal Model:Female NOD-SCID mouse (6?7 weeks old) Dosage:20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus 5% DMSO, administered at a dose of 5 mL/kg Administration:Intraperitoneal injection; once daily; 21 days Result:Inhibited tumor growth by 66% and 84% at concentration of 20 mg/kg and 40 mg/kg, respectively.Resulted cell proliferation inhibition and apoptosis induction.

SKLB4771 | SKLB-4771 | SKLB 4771. FLT3-IN-1

Angiogenesis

FLT

FLT3

Cancer

——

1370256-78-2

537.66

C25H27N7O3S2

>98% (HPLC)

DMSO: 10 mM

O=C(NC1=CC=C(C)C=C1)NC2=NN=C(SC3=C4C=CC(OCCCN5CCOCC5)=CC4=NC=N3)S2

1-{5-[7-(3- Morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea

(-20℃)

With Ice Pack

≥ 2 years