JH-VIII-157-02
Names
[ CAS No. ]:
1639422-97-1
[ Name ]:
JH-VIII-157-02
Biological Activity
[Description]:
JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
[Related Catalog]:
[Target]
IC50: 2 nM (EML4-ALK G1202R, cell assay), 2 nM (EML4-ALKwt, cell assay), 2 nM (EML4-ALK C1156Y, cell assay), 2 nM (EML4-ALK F1174L, cell assay), 2 nM (EML4-ALK F1174L, cell assay)[1]
[In Vitro]
JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALKwt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC50, 2 nM), EAG1269A (IC50, 3 nM), EAL1196M (IC50, 58 nM), EA1151Tins (IC50, 107 nM), and EAL1152R (IC50, 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC50s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC50s of 5, 19 nM, respectively[1].
[In Vivo]
JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice[1].
[Cell Assay]
Cells are seeded at 4000 per well in 96 well plates and exposed to JH-VIII-157-02 in triplicate at 1 nM to 10 μM for 72 hours. Cell viability is evaluated using CellTiter-Glo Luminescent Cell Viability Assay. IC50 values are calculated by nonlinear regression (variable slope) using GraphPad Prism 5 software. Each experiment is repeated for at least twice[1].
[References]
[Related Small Molecules]
Brigatinib
|
lorlatinib
|
Alectinib (CH5424802)
|
Entrectinib
|
TAE684(NVP-TAE684)
|
AZD-3463
|
Repotrectinib
|
Ensartinib
|
AP26113
|
K 02288
|
ASP3026
|
CEP-37440
|
GSK1838705A
|
Belizatinib
Chemical & Physical Properties
[ Molecular Formula ]:
C28H27N5O2
[ Molecular Weight ]:
465.55
[ Storage condition ]:
2-8℃