DC-120
DC-120 is an ATP competitive AKT kinase inhibitor that suppressed proliferation and induced apoptosis in liver cancer cells both in vitro and in vivo. DC120 blocked the phosphorylation of downstream molecules in the AKT signal pathway in dose- and time-dependent manners both in vitro and in vivo. DC120 inhibits AKT activity in vitro with an EC(50) of 153 nM. DC120 at 20 mg/kg/day inhibited the CNE2 xenograft tumor growth with a treated group/control group ratio of 38.1%, accompanied by increasing terminal deoxynucleotidyl transferasedUTP nick-end labeling-positive cells in the tumor sample.
1: Yang F, Deng R, Qian XJ, Chang SH, Wu XQ, Qin J, Feng GK, Ding K, Zhu XF. Feedback loops blockade potentiates apoptosis induction and antitumor activity of a novel AKT inhibitor DC120 in human liver cancer. Cell Death Dis. 2014 Mar 13;5:e1114. doi: 10.1038/cddis.2014.43. PubMed PMID: 24625973; PubMed Central PMCID: PMC3973233.
2: Deng R, Yang F, Chang SH, Tang J, Qin J, Feng GK, Ding K, Zhu XF. DC120, a novel and potent inhibitor of AKT kinase, induces tumor cell apoptosis and suppresses tumor growth. Mol Pharmacol. 2012 Aug;82(2):189-98. doi: 10.1124/mol.111.077271. Epub 2012 May 2. PubMed PMID: 22553359.
2: Deng R, Yang F, Chang SH, Tang J, Qin J, Feng GK, Ding K, Zhu XF. DC120, a novel and potent inhibitor of AKT kinase, induces tumor cell apoptosis and suppresses tumor growth. Mol Pharmacol. 2012 Aug;82(2):189-98. doi: 10.1124/mol.111.077271. Epub 2012 May 2. PubMed PMID: 22553359.
| Chemical | |
|---|---|
| CAS Num | 1261080-40-3 |
| Chemical Formula | C18H18Cl2N6OS |
| Molecular Weight | 437.35 |
| IUPAC Chemical Name | (S)-N-(1-amino-3-(2,4-dichlorophenyl)propan-2-yl)-2-(2-(methylamino)pyrimidin-4-yl)thiazole-5-carboxamide |
| Exact Mass | 436.06399 |
| Elemental Analysis | C, 49.43; H, 4.15; Cl, 16.21; N, 19.22; O, 3.66; S, 7.33 |
| Synonym | DC120; DC 120; DC120. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(C1=CN=C(C2=NC(NC)=NC=C2)S1)N[C@@H](CC3=CC=C(Cl)C=C3Cl)CN |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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