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JAK3 INHIBITOR VI

Product Name
JAK3 INHIBITOR VI
CAS No.
856436-16-3
Chemical Name
JAK3 INHIBITOR VI
Synonyms
JI6;JAK3 INHIBITOR VI
CBNumber
CB3787012
Molecular Formula
C19H17N3O4S
Formula Weight
383.42098
MOL File
856436-16-3.mol
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JAK3 INHIBITOR VI Property

storage temp. 
+2C to +8C
form 
Yellow solid
color 
yellow
Water Solubility 
water: 1mg/mL
DMSO: 5mg/mL
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
420126
Product name
JAK3 Inhibitor VI - CAS 856436-16-3 - Calbiochem
Packaging
5MG
Price
$176
Updated
2025/07/31
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JAK3 INHIBITOR VI Chemical Properties,Usage,Production

Uses

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].

General Description

A cell-permeable, potent, and reversible inhibitor of Janus kinase 3 (JAK3) (IC50 = 27 nM). Reported to bind to the enzyme active site and prevent IL-2-induced phosphorylation of JAK3 and STAT5. Also reported to inhibit IL-2-induced cell proliferation (IC50 = 760 nM for murine CTLL cells and 250 nM for human T-cells). Shown to alleviate oxazolone-induced ear edema in mice with an efficacy comparable to Dexamethasone (Cat. No. 265005) and displays ~16-fold greater selectivity over JAK2.

Biochem/physiol Actions

Cell permeable: yes

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].

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.

IC 50

FLT3-D835H: 4 nM (IC50); FLT3-D835Y: 8 nM (IC50); FLT3-WT: 40 nM (IC50); JAK3: ~250 nM (IC50); c-Kit: ~500 nM (IC50)

References

[1] Chen Y, et, al. Identification of an orally available compound with potent and broad FLT3 inhibition activity. Oncogene. 2016 Jun 9;35(23):2971-8. DOI:10.1038/onc.2015.362

JAK3 INHIBITOR VI Preparation Products And Raw materials

Raw materials

Preparation Products

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JAK3 INHIBITOR VI Suppliers

China 15 United States 3 Global 18
SHANGHAI FORTUNE CHEMICAL TECHNOLOGY CO., LTD
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856436-16-3, JAK3 INHIBITOR VIRelated Search:


  • JAK3 INHIBITOR VI
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