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.
Compound Libraries
KRCA 0008 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 609.12 |
| Formula | C30H37ClN8O4 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1472795-20-2 |
| PubChem ID | 72547474 |
| InChI Key | TXDIRJCYNAWBOS-UHFFFAOYSA-N |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 60.91 | 100 | |
| DMSO | 60.91 | 100 | |
| ethanol | 60.91 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 609.12. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 |
Molarity Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
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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