CA-224
CA-224 is potent CDK4 inhibitor, is also a nonplanar analogue of fascaplysin that specifically inhibits Cdk4-cyclin D1 in vitro. CA-224 blocks the growth of cancer cells at G0/ G1 phase of the cell cycle. CA-224 also blocks the cell cycle at G2/M phase, which is explained by the fact that it inhibits tubulin polymerization. Additionally, CA-224 acts as an enhancer of depolymerization for taxol-stabilized tubulin. CA-224 selectively induces apoptosis of SV40 large Tantigen. transformed cells and significantly reduces colony formation efficiency, in a dose-dependent manner, of lung cancer cells. The promising efficacy of CA-224 in human xenograft models as well as its excellent therapeutic window indicates its potential for clinical development.
1: Mahale S, Aubry C, James Wilson A, Jenkins PR, Maréchal JD, Sutcliffe MJ, Chaudhuri B. CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4272-8. Epub 2006 Jun 5. PubMed PMID: 16750360.
2: Webb J. Estimating the potential for ammonia emissions from livestock excreta and manures. Environ Pollut. 2001;111(3):395-406. PubMed PMID: 11202744.
2: Webb J. Estimating the potential for ammonia emissions from livestock excreta and manures. Environ Pollut. 2001;111(3):395-406. PubMed PMID: 11202744.
| Chemical | |
|---|---|
| CAS Num | 883561-04-4 |
| Chemical Formula | C24H22N2O |
| Molecular Weight | 354.4443 |
| IUPAC Chemical Name | N-(2-(1H-indol-3-yl)ethyl)-N-methyl-[1,1'-biphenyl]-4-carboxamide |
| Exact Mass | 354.1732 |
| Elemental Analysis | C, 81.33; H, 6.26; N, 7.90; O, 4.51 |
| Synonym | CA224; CA 224; CA-224. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N(CCC3=CNC4=C3C=CC=C4)C |
| Biological | |
| Targets and Effects | CDK4 inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | 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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