KRCA 0008

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Description: Potent Ack1 and ALK dual inhibitor; orally bioavailable
Chemical Name: 1,1'-[(5-Chloro-2,4-pyrimidinediyl)bis[imino(3-methoxy-4,1-phenylene)-4,1-piperazinediyl]]bisethanone
Purity: ≥99% (HPLC)

Biological Activity for KRCA 0008

KRCA 0008 is a 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 for KRCA 0008

M. Wt 609.12
Formula C30H37ClN8O4
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1472795-20-2
PubChem ID 72547474
Smiles ClC1=C(NC2=C(OC)C=C(N3CCN(C(C)=O)CC3)C=C2)N=C(NC4=CC=C(N5CCN(C(C)=O)CC5)C=C4OC)N=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KRCA 0008

Solvent Max Conc. mg/mL Max Conc. mM
1eq. HCl 60.91 100
DMSO 60.91 100
ethanol 60.91 100

Preparing Stock Solutions for KRCA 0008

The following data is based on the product molecular weight 609.12. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.64 mL 8.21 mL 16.42 mL
5 mM 0.33 mL 1.64 mL 3.28 mL
10 mM 0.16 mL 0.82 mL 1.64 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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References for KRCA 0008

References are publications that support the biological activity of the product.

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

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

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