JI6

SKU: orb1819235

Description

JI6 is a potent, selective, and orally bioavailable small molecule inhibitor primarily targeting FLT3 (IC50 ~40 nM WT), with additional activity against c-Kit and JAK3. It is a valuable research tool for studying acute myeloid leukemia, demonstrating efficacy in both cellular assays and in vivo models of FLT3-driven disease.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 856436-16-3
• MW: 383.42
• Purity: 98.64%
• Formula: C₁₉H₁₇N₃O₄S
• SMILES: CS(=O)(O)=O.O=C(/C1=C\C2=CC=CN2)NC(C=C3)=C1C=C3C4=CN=CC=C4
• Target: JAK,FLT,c-Kit
• Solubility: DMSO:4.5 mg/mL (11.74 mM)

Bioactivity

• Target IC50:
  FLT3 (D835H):4 nM|FLT3 (WT):40 nM|FLT3 (D835Y):8 nM|JAK3:~250 nM|c-Kit:~500 nM
• In Vivo:
  JI6 (15 mg/kg; i.p. daily for 3 weeks) inhibits the proliferation of HCD-57 expressing FLT3-D835Y in SCID mice and prolongs survival. JI6 (25 mg/kg; p.o. daily for 3 weeks) inhibits the myeloproliferative phenotype in FLT3-ITD knock-in mice. JI6 (100 mg/kg; a single i.p.) significantly inhibits FLT3 phosphorylation and downstream signal transduction in mice expressing FLT3-D835Y.
• In Vitro:
  JI6 (3-1000 nM; 1-4 days) inhibits MV4-11 cell viability dose-dependently with an IC50 of ∼25 nM. It also potently inhibits the viability of HCD-57 cells expressing FLT3-ITD, FLT3-D835Y, and FLT3-D835H (1-2000 nM; 48 h) with an IC50 of ∼40 nM, while showing no effect on parent HCD-57 or JAK2V617F expressing cells. Additionally, JI6 (100-500 nM; 24 h) induces apoptosis and cell cycle arrest, and (50-500 nM; 3 h) inhibits phosphorylation of FLT3, ERK, and Akt in HCD-57 cells expressing FLT3-ITD and FLT3-D835Y.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JI 6, JI6, JI-6, JAK3 Inhibitor VI, FLT3

Compound Identifiers

PubChem CID

16760524