| Identification | Back Directory | [Name]
JH-VIII-157-02 | [CAS]
1639422-97-1 | [Synonyms]
JH-VIII-157-02
1H-Pyrazole-1-acetamide, 4-(3-cyano-9-ethyl-6,11-dihydro-6,6-dimethyl-11-oxo-5H-benzo[b]carbazol-8-yl)-N,N-dimethyl- | [Molecular Formula]
C28H27N5O2 | [MDL Number]
MFCD31657417 | [MOL File]
1639422-97-1.mol | [Molecular Weight]
465.55 |
| Chemical Properties | Back Directory | [Boiling point ]
751.9±60.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 25 mg/mL (53.70 mM) | [form ]
Solid | [pka]
13.70±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
JH-VIII-157-02, a structural analog of alectinib, is an ALK inhibitor with IC50 of 2 nM for echinoderms microtubule-associated protein-like 4 (EML4)-ALK G1202R. | [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. | [target]
IC50: 2 nM (EML4-ALK G1202R, cell assay), 2 nM (EML4-ALK wt , cell assay), 2 nM (EML4-ALK C1156Y, cell assay) , 2 nM (EML4-ALK F1174L, cell assay), 2 nM (EML4-ALK F1174L, cell assay) | [storage]
Store at -20°C | [References]
[1] Hatcher JM, et al. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308. DOI:10.1021/acs.jmedchem.5b01136 |
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