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.
Product information
CAS Number: 1639422-97-1
Molecular Weight: 465.55
Formula: C28H27N5O2
Chemical Name: 2-(4-{3-cyano-9-ethyl-6,6-dimethyl-11-oxo-5H,6H,11H-benzo[b]carbazol-8-yl}-1H-pyrazol-1-yl)-N,N-dimethylacetamide
Smiles: CN(C)C(=O)CN1C=C(C=N1)C1C=C2C(=CC=1CC)C(=O)C1=C(NC3C=C(C=CC=31)C#N)C2(C)C
InChiKey: IDGNCVHQDDOPND-UHFFFAOYSA-N
InChi: InChI=1S/C28H27N5O2/c1-6-17-10-21-22(11-20(17)18-13-30-33(14-18)15-24(34)32(4)5)28(2,3)27-25(26(21)35)19-8-7-16(12-29)9-23(19)31-27/h7-11,13-14,31H,6,15H2,1-5H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 25 mg/mL (53.70 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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