Benzamide, N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-
Volasertib (BI 6727)
CAS: 755038-65-4
Molecular Formula: C34H50N8O3
Benzamide, N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy- - Names and Identifiers
Benzamide, N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy- - Physico-chemical Properties
| Molecular Formula | C34H50N8O3 |
| Molar Mass | 618.81 |
| Density | 1.26 |
| Melting Point | 86 - 87*C |
| Solubility | Soluble in DMSO, not in water |
| Appearance | solid |
| Color | Off-white |
| pKa | 14.26±0.40(Predicted) |
| Storage Condition | -20° |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| In vitro study | Like BI2536,BI6727 is an ATP competitive kinase inhibitor belonging to the dihydropteridinone class of compounds. In addition to Plk1,BI6727 also potently inhibits two closely related kinases, Plk2 and Plk3, with IC50 of 5 nM and 56 nM, respectively. BI6727 has no inhibitory activity on more than fifty kinases at concentrations up to 10 μm. BI6727 inhibits the proliferation of multiple cell lines derived from various cancer tissues, including HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1 and Raji cells, with EC50 of 23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM and 37 nM. In NCI-H460 cells, BI6727 (100 nM) induced aggregation of mitotic cells with unipolar spindles and positive staining for phosphoserine 10 of histone H3, which indicated that the cells were in M-phase, apoptosis is subsequently induced. Low nanomolar concentration of BI6727 showed inhibitory activity on neuroblastoma (NB) tumor-initiating cells (NB TIC), with EC 50 of 21 nM, only micromolar concentrations of BI6727 have toxic effects on normal pediatric neural stem cells. Similar to BI2536,BI6727 induced growth arrest of Daoy and ONS-76 medulloblastoma cells. |
| In vivo study | BI6727 significantly inhibits the growth of multiple human tumor xenografts, including HCT116, NCI-H460, and taxane-resistant CXB1 colon cancers, with increased mitotic index and increased apoptosis. In vivo studies have shown that BI6727 exhibits better toxicity and pharmacokinetic profiles than bi2536. |
Benzamide, N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy- - Reference
| Reference Show more | 1: Stadler WM, Vaughn DJ, Sonpavde G, Vogelzang NJ, Tagawa ST, Petrylak DP, Rosen P, Lin CC, Mahoney J, Modi S, Lee P, Ernstoff MS, Su WC, Spira A, Pilz K, Vinisko R, Schloss C, Fritsch H, Zhao C, Carducci MA. An open-label, single-arm, phase 2 trial of the polo-like kinase inhibitor volasertib (BI 6727) in patients with locally advanced or metastatic urothelial cancer. Cancer. 2013 Dec 11. doi: 10.1002/cncr.28519. [Epub ahead of print] PubMed PMID: 24339028. 2: Danovi D, Folarin A, Gogolok S, Ender C, Elbatsh AM, Engström PG, Stricker SH, Gagrica S, Georgian A, Yu D, U KP, Harvey KJ, Ferretti P, Paddison PJ, Preston JE, Abbott NJ, Bertone P, Smith A, Pollard SM. A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1. PLoS One. 2013 Oct 30;8(10):e77053. doi: 10.1371/journal.pone.0077053. eCollection 2013. PubMed PMID: 24204733; PubMed Central PMCID: PMC3813721. 3: Gorlick R, Kolb EA, Keir ST, Maris JM, Reynolds CP, Kang MH, Carol H, Lock R, Billups CA, Kurmasheva RT, Houghton PJ, Smith MA. Initial testing (stage 1) of the Polo-like kinase inhibitor volasertib (BI 6727), by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2014 Jan;61(1):158-64. doi: 10.1002/pbc.24616. Epub 2013 Aug 19. PubMed PMID: 23956067. |
Benzamide, N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.616 ml | 8.08 ml | 16.16 ml |
| 5 mM | 0.323 ml | 1.616 ml | 3.232 ml |
| 10 mM | 0.162 ml | 0.808 ml | 1.616 ml |
| 5 mM | 0.032 ml | 0.162 ml | 0.323 ml |
Last Update：2024-01-02 23:10:35
![Benzamide, N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-](http://res.chembk.com/assets/str/2d/7/75/755038-65-4.png)
Supplier List
Product Name: Volasertib (BI 6727) Visit Supplier Webpage Request for quotation
CAS: 755038-65-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 755038-65-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: Volasertib (BI 6727) Visit Supplier Webpage Request for quotation
CAS: 755038-65-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 755038-65-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History