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JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $163 | In Stock | |
5 mg | $379 | In Stock | |
10 mg | $568 | In Stock | |
25 mg | $913 | In Stock | |
50 mg | $1,230 | In Stock | |
100 mg | $1,680 | In Stock | |
500 mg | $3,360 | In Stock |
Description | JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia. |
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[1]. |
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[1]. |
Alias | JAK3 Inhibitor VI |
Molecular Weight | 383.42 |
Formula | C19H17N3O4S |
Cas No. | 856436-16-3 |
Smiles | CS(=O)(O)=O.O=C(/C1=C\C2=CC=CN2)NC(C=C3)=C1C=C3C4=CN=CC=C4 |
Relative Density. | no data available |
Storage | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.5 mg/mL (11.7 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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