[CAS NO. 856436-16-3] JI6
PRODUCTS SPECIFICATIONS [856436-16-3]
DESCRIPTION [856436-16-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 383.42 |
| Molecular Formula | C19H17N3O4S |
| SMILES | O=C1NC2=CC=C(C3=CN=CC=C3)C=C2/C1=C/C4=CC=CN4.O=S(O)(C)=O |
Summary
IC50 & Target
|
FLT3-D835H 4 nM (IC 50 ) |
FLT3-D835Y 8 nM (IC 50 ) |
FLT3-WT 40 nM (IC 50 ) |
JAK3 ~250 nM (IC 50 ) |
c-Kit ~500 nM (IC 50 ) |
In Vitro
JI6 (3-1000 nM; 1-4 days) selectively inhibits the viability of MV4-11 cells in a dose-dependent manner, with an IC
50
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 IC
50
s 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
