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KRCA-0008

Chemical Structure : KRCA-0008

CAS No.: 1472795-20-2

KRCA-0008 (KRCA 0008, KRCA0008)

Catalog No.: PC-42979Not For Human Use, Lab Use Only.

KRCA-0008 is a potent, selective ALK inhibitor with IC50 of 12 nM (wt ALK), also is potent against various ALK mutants, including L1196M, F1174L, R1275Q, and C1156Y (IC50=5-75 nM).

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

Biological Activity

KRCA-0008 is a potent, selective ALK inhibitor with IC50 of 12 nM (wt ALK), also is potent against various ALK mutants, including L1196M, F1174L, R1275Q, and C1156Y (IC50=5-75 nM).
KRCA-0008 weakly inhibits IR (IC50=210 nM), inhibits H3122 and BaF3 EML4-ALK L1196M cell proliferation with IC50 of 80 and 68 nM, respectively.
KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model, has drug-like properties without hERG concerns.

Physicochemical Properties

M.Wt 609.119
Formula C30H37ClN8O4
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

Ethanone, 1,1'-[(5-chloro-2,4-pyrimidinediyl)bis[imino(3-methoxy-4,1-phenylene)-4,1-piperazinediyl]]bis-

References

1. Park CH, et al. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6.

2. Kang CH, et al. Biochem Biophys Res Commun. 2015 Aug 28;464(3):762-7.

3. Lee HJ, et al. Arch Pharm Res. 2014;37(9):1130-8.

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