1. Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
    JAK/STAT Signaling
    Epigenetics
  2. FLT3
    JAK
    c-Kit
  3. JI6

JI6 

Cat. No.: HY-18949
Handling Instructions

JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.

For research use only. We do not sell to patients.

JI6 Chemical Structure

JI6 Chemical Structure

CAS No. : 856436-16-3

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Description

JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

FLT3-D835H

4 nM (IC50)

FLT3-D835Y

8 nM (IC50)

FLT3-WT

40 nM (IC50)

JAK3

~250 nM (IC50)

c-Kit

~500 nM (IC50)

In Vitro

JI6 (3-1000 nM; 1-4 days) selectively inhibits the viability of MV4-11 cells in a dose-dependent manner, with an IC50 of ∼25 nM[1].
JI6 (1-2000 nM; 48 h) potently inhibits the viability of HCD-57 cells expressing FLT3-ITD, FLT3-D835Y, and FLT3-D835H with IC50s of ∼40 nM, but it displays essentially no effects on the parent HCD-57 or the cells transformed with JAK2V617F[1].
JI6 (100-500 nM; 24 h) induces apoptosis and cell cycle arrest in both FLT3-ITD- and FLT3-D835Y-expressing HCD-57 cells[1].
JI6 (50-500 nM; 3 h) inhibits phosphorylation of FLT3 and its downstream signaling transducers including ERK and Akt in FLT3-ITD- and FLT3-D835Y-transfromed HCD-57 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MV4-11, HL60, Karpas 299, and Jurkat cells
Concentration: 3-1000 nM
Incubation Time: 48 hours
Result: Inhibited MV4-11 cells and no effects of JI6 on the three remaining cells at a concentration as high as 1 μM.

Apoptosis Analysis[1]

Cell Line: FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
Concentration: 100, 500 nM
Incubation Time: 24 hours
Result: Increased the percentage of apoptotic and necrotic cells and displayed no effects on the apoptosis of the parent HCD-57 cells.

Cell Cycle Analysis[1]

Cell Line: FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
Concentration: 100, 500 nM
Incubation Time: 24 hours
Result: Significantly reduced G2 and S phase cells and increased G1 phase cells in both FLT3-ITD and D835Y cells.

Cell Viability Assay[1]

Cell Line: FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
Concentration: 50, 100, 500 nM
Incubation Time: 3 hours
Result: Inhibited phosphorylation of FLT3, ERK1, ERK2 and Akt.
In Vivo

JI6 (15 mg/kg; i.p. daily for 3 weeks) inhibits the proliferation of FLT3-D835Y-transformed HCD-57 in immunodeficient mice and prolongs the mice survival[1].
JI6 (25 mg/kg; p.o. daily for 3 weeks) suppresses myeloproliferative phenotypes in FLT3-ITD knock-in mice[1].
JI6 (100 mg/kg; a single i.p.) significantly inhibits phosphorylation of FLT3 and downstream signal transductionin mice expressing FLT3-D835Y[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG mice (10-12 weeks old, male) were implanted with FLT3-D835Y-transformed HCD-57 cells[1]
Dosage: 15 mg/kg
Administration: I.p. daily for 3 weeks
Result: Reduced the spleen size and prolonged the survival of these mice.
Molecular Weight

383.42

Formula

C19H17N3O4S

CAS No.
SMILES

O=C1NC2=CC=C(C3=CN=CC=C3)C=C2/C1=C/C4=CC=CN4.O=S(O)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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