JI6
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.
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- No. CAS: 856436-16-3
- Fòrmula: C19H17N3O4S
- Peso molecular:383.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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FLT3-D835H 4 nM (IC50) |
FLT3-D835Y 8 nM (IC50) |
FLT3-WT 40 nM (IC50) |
JAK3 ~250 nM (IC50) |
c-Kit ~500 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11, HL60, Karpas 299, and Jurkat cells
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Concentration:3-1000 nM
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Incubation Time:48 hours
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Result:Inhibited MV4-11 cells and no effects of JI6 on the three remaining cells at a concentration as high as 1 μM.
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Cell Line:FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
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Concentration:100, 500 nM
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Incubation Time:24 hours
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Result:Increased the percentage of apoptotic and necrotic cells and displayed no effects on the apoptosis of the parent HCD-57 cells.
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Cell Line:FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
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Concentration:100, 500 nM
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Incubation Time:24 hours
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Result:Significantly reduced G2 and S phase cells and increased G1 phase cells in both FLT3-ITD and D835Y cells.
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Cell Line:FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
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Concentration:50, 100, 500 nM
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Incubation Time:3 hours
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Result:Inhibited phosphorylation of FLT3, ERK1, ERK2 and Akt.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (10-12 weeks old, male) were implanted with FLT3-D835Y-transformed HCD-57 cells[1]
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Dosage:15 mg/kg
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Administration:I.p. daily for 3 weeks
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Result:Reduced the spleen size and prolonged the survival of these mice.
Chemical Information
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No. CAS 856436-16-3
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Peso molecular 383.42
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Fòrmula C19H17N3O4S
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SMILES
O=C1NC2=CC=C(C3=CN=CC=C3)C=C2/C1=C/C4=CC=CN4.O=S(O)(C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JI6 Related Classifications
HY-18949 Related Classifications
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