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JH-VIII-157-02

Chemical Structure : JH-VIII-157-02

CAS No.: 1639422-97-1

JH-VIII-157-02 (ALK G1202R inhibitor)

Catalog No.: PC-35352Not For Human Use, Lab Use Only.

JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y).
JH-VIII-157-02 inhibits EML4-ALKWT with IC50 of 2 nM, demonstrates inhibition of CSNK2A1 <10 uM, IRAK1 (IC50 =14 nM), IRAK4 with (IC50=465 nM), CLK4 (IC50=14 nM), RET (IC50=3 nM), RET V804L (IC50=13 nM).
JH-VIII-157-02 potently inhibits proliferation of NSCLC H3122 cell line with IC50 of 5 nM.

Physicochemical Properties

M.Wt 465.557
Formula C28H27N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-(3-cyano-9-ethyl-6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazol-8-yl)-1H-pyrazol-1-yl)-N,N-dimethylacetamide

References

1. Hatcher JM, et al. J Med Chem. 2015 Dec 10;58(23):9296-9308.

2. Wang H, et al. Drug Des Devel Ther. 2018 May 9;12:1183-1193.

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