BPR1K653
BPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats., BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments.
1: Cheung CH, Lin WH, Hsu JT, Hour TC, Yeh TK, Ko S, Lien TW, Coumar MS, Liu JF, Lai WY, Shiao HY, Lee TR, Hsieh HP, Chang JY. BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells. PLoS One. 2011;6(8):e23485. doi: 10.1371/journal.pone.0023485. Epub 2011 Aug 24. PubMed PMID: 21887256; PubMed Central PMCID: PMC3160846.
| Chemical | |
|---|---|
| CAS Num | 1192754-07-6 (BPR1K653 HCl salt) |
| Chemical Formula | C30H29ClN6O2 |
| Molecular Weight | 541.04 |
| IUPAC Chemical Name | 1-(4-(2-((5-chloro-6-phenylfuro[2,3-d]pyrimidin-4-yl)amino)ethyl)phenyl)-3-(2-((dimethylamino)methyl)phenyl)urea |
| Exact Mass | 540.20405 |
| Elemental Analysis | C, 66.60; H, 5.40; Cl, 6.55; N, 15.53; O, 5.91 |
| Synonym | BPR1K653; BPR1K 653; BPR1K-653. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(NC1=CC=CC=C1CN(C)C)NC2=CC=C(CCNC3=C4C(OC(C5=CC=CC=C5)=C4Cl)=NC=N3)C=C2 |
| Biological | |
| Targets and Effects | Aurora kinase 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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