KRCA 0008

Cat. No. 5098

KRCA 0008 C30H37ClN8O4 [1472795-20-2]

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Chemical Name: 1,1'-[(5-Chloro-2,4-pyrimidinediyl)bis[imino(3-methoxy-4,1-phenylene)-4,1-piperazinediyl]]bisethanone

Biological Activity

Potent Ack1 and anaplastic lymphoma kinase (ALK) dual inhibitor (IC50 values are 4 and 12 nM respectively). Inhibits lung cancer H3122 cell proliferation (IC50 = 80 nM). Attenuates H3122 cell xenograft tumor growth in mice. Orally bioavailable.

Technical Data

M.Wt:
609.12
Formula:
C30H37ClN8O4
Solubility:
Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>99 %
Storage:
Store at -20°C
CAS No:
1472795-20-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Lee et al (2014) ALK inhibitors of bis-ortho-alkoxy-para-piperazinesubstituted-pyrimidines and -triazines for cancer treatment. Arch.Pharm.Res. 37 1130. PMID: 24446111.

Park et al (2013) Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg.Med.Chem.Lett. 23 6192. PMID: 24095090.

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Keywords: KRCA 0008, supplier, KRCA0008, Potent, anaplastic, lymphoma, kinase, ALK, Ack1, inhibitors, inhibits, antitumor, tyrosine, kinases, orally, bioavailable, TNK2, Tocris Bioscience, ALK Inhibitor products

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