FLT3-IN-1

SKU: orb1226429

Description

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.

Key Properties

• CAS Number: 1370256-78-2
• MW: 537.66
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₇N₇O₃S₂
• SMILES: O=C(NC1=CC=C(C)C=C1)NC2=NN=C(SC3=C4C=CC(OCCCN5CCOCC5)=CC4=NC=N3)S2
• Target: FLT
• Solubility: DMSO: 10 mM

Bioactivity

• 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.). 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.
• 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Quick Database Links

Gene Symbol

FLT