Bulk Inquiry
KRCA 0008
- Soluble in DMSO
- MF: C30H37ClN8O4
- MW: 609.12
Description
Potent and selective dual ALK (anaplastic lymphoma kinase ) and ACK1 inhibitor (IC50 values 12 nM and 4 nM for ALK and Ack1, respectively) with good drug-like properties: good water-solubility with moderate plasma protein binding and low brain exposure. It has good liver microsomal stability and little to no CYP inhibition. KRCA0008 also shows promising pharmacokinetic parameters in both mice and rat (oral bioavailability = 66-94.5%) and a modest tumor growth inhibition in vivo activity in H3122 human lung cancer bearing mice model comparable to Crizotinib (Axon 1660) without significant body weight change.
More Information
| Parent CAS No. | 1472795-20-2 |
|---|---|
| Chemical Name | 1,1'-(4,4'-(4,4'-(5-chloropyrimidine-2,4-diyl)bis(azanediyl)bis(3-methoxy-4,1-phenylene))bis(piperazine-4,1-diyl))diethanone |
| SMILES | C1(NC2=CC=C(N3CCN(C(=O)C)CC3)C=C2OC)=NC=C(Cl)C(NC2=CC=C(N3CCN(C(=O)C)CC3)C=C2OC)=N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C30H37ClN8O4/c1-20(40)36-9-13-38(14-10-36)22-5-7-25(27(17-22)42-3)33-29-24(31)19-32-30(35-29)34-26-8-6-23(18-28(26)43-4)39-15-11-37(12-16-39)21(2)41/h5-8,17-19H,9-16H2,1-4H3,(H2,32,33,34,35) |
| InChiKey | TXDIRJCYNAWBOS-UHFFFAOYSA-N |
| CID | 72547474 |
| Short Description | Dual ACK1/ALK inhibitor |
References
- C.H. Park et al. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6.
- H.J. Lee et al. ALK inhibitors of bis-ortho-alkoxy-para-piperazinesubstituted-pyrimidines and -triazines for cancer treatment. Arch Pharm Res. 2014 Sep;37(9):1130-8.
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