CFI-400945 fumarate
CFI-400945 is an orally available fumarate salt form of CFI-400945, a polo-like kinase 4 (PLK4) inhibitor with potential antineoplastic activity. Upon oral administration, polo-like kinase 4 inhibitor CFI-400945 selectively inhibits PLK4, which results in the disruption of mitosis and the induction of apoptosis. PLK4 inhibition also prevents cell division and inhibits proliferation of PLK4-overexpressing tumor cells. PLK4, a member of the polo family of serine/threonine kinases overexpressed in a variety of cancer cell types, plays a crucial role in the regulation of centriole duplication during the cell cycle.
1: Yu B, Yu Z, Qi PP, Yu Q, Liu HM. Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: Success and challenges. Eur J Med Chem. 2015 Mar 12;95:35-40. doi: 10.1016/j.ejmech.2015.03.020. [Epub ahead of print] PubMed PMID: 25791677.
2: Sampson PB, Liu Y, Forrest B, Cumming G, Li SW, Patel NK, Edwards L, Laufer R, Feher M, Ban F, Awrey DE, Mao G, Plotnikova O, Hodgson R, Beletskaya I, Mason JM, Luo X, Nadeem V, Wei X, Kiarash R, Madeira B, Huang P, Mak TW, Pan G, Pauls HW. The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5Â
2: Sampson PB, Liu Y, Forrest B, Cumming G, Li SW, Patel NK, Edwards L, Laufer R, Feher M, Ban F, Awrey DE, Mao G, Plotnikova O, Hodgson R, Beletskaya I, Mason JM, Luo X, Nadeem V, Wei X, Kiarash R, Madeira B, Huang P, Mak TW, Pan G, Pauls HW. The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5Â
| Chemical | |
|---|---|
| CAS Num | 1616420-30-4 (CFI-400945 fumarate) |
| Chemical Formula | C37H38N4O7 |
| Molecular Weight | 650.72 |
| IUPAC Chemical Name | (1R,2S)-2-(3-((E)-4-(((2S,6R)-2,6-dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one fumarate |
| Elemental Analysis | C, 68.29; H, 5.89; N, 8.61; O, 17.21 |
| Synonym | CFI400945; CFI 400945; CFI-400945; CFI-400945 fumarate. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(NC1=C2C=C(C=C1)OC)[C@@]32[C@@H](C3)C4=CC5=C(C(/C=C/C6=CC=C(C=C6)CN7C[C@@H](O[C@@H](C7)C)C)=NN5)C=C4.O=C(O)/C=C/C(O)=O |
| Biological | |
| Targets and Effects | N/A |
| 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 |
Mailing Address
Anba Pharma Company
3-H Gill Street, Suite 300
Woburn, MA 01801
United State
Our Contact Info.
Tel: 1+610-883-0668
Email: sales@AnbaPharma.com