Volasertib
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MedKoo CAT#: 200494

CAS#: 755038-65-4

Description: Volasertib, also known as BI-6727, is a dihydropteridinone Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. BI 6727 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. BI 6727 is highly potent (enzyme IC(50) = 0.87 nmol/L, EC(50) = 11-37 nmol/L on a panel of cancer cell lines) and selective dihydropteridinone with distinct properties.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 850
1g
USD 2950
Size
Price

25mg
USD 250
200mg
USD 1250
2g
USD 3950
Size
Price

50mg
USD 450
500mg
USD 1950
5g
Ask price

Volasertib (BI6727), purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 500mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 200494
Name: Volasertib
CAS#: 755038-65-4
Chemical Formula: C34H50N8O3
Exact Mass: 618.40059
Molecular Weight: 618.8126
Elemental Analysis: C, 65.99; H, 8.14; N, 18.11; O, 7.76


Synonym: BI6727, BI-6727, BI 6727, Volasertib

IUPAC/Chemical Name: N-((1s,4S)-4-(4-(cyclopropylmethyl)piperazin-1-yl)cyclohexyl)-4-(((R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxybenzamide

InChi Key: SXNJFOWDRLKDSF-FULLSBAXSA-N

InChi Code: InChI=1S/C34H50N8O3/c1-6-28-33(44)39(4)29-20-35-34(38-31(29)42(28)22(2)3)37-27-14-9-24(19-30(27)45-5)32(43)36-25-10-12-26(13-11-25)41-17-15-40(16-18-41)21-23-7-8-23/h9,14,19-20,22-23,25-26,28H,6-8,10-13,15-18,21H2,1-5H3,(H,36,43)(H,35,37,38)/t25-,26+,28-/m1/s1

SMILES Code: O=C(N[C@H]1CC[C@@H](N2CCN(CC3CC3)CC2)CC1)C4=CC=C(NC(N=C5N(C(C)C)[C@@H]6CC)=NC=C5N(C)C6=O)C(OC)=C4


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner.


References

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.

4: Krause M, Kummer B, Deparade A, Eicheler W, Pfitzmann D, Yaromina A, Kunz-Schughart LA, Baumann M. Simultaneous PLK1 inhibition improves local tumour control after fractionated irradiation. Radiother Oncol. 2013 Sep;108(3):422-8. doi: 10.1016/j.radonc.2013.06.038. Epub 2013 Jul 25. PubMed PMID: 23891096.

5: Pezuk JA, Brassesco MS, Morales AG, de Oliveira JC, de Paula Queiroz RG, Machado HR, Carlotti CG Jr, Neder L, Scrideli CA, Tone LG. Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma. Cancer Gene Ther. 2013 Sep;20(9):499-506. doi: 10.1038/cgt.2013.46. Epub 2013 Jul 26. PubMed PMID: 23887645.

6: Wissing MD, Mendonca J, Kortenhorst MS, Kaelber NS, Gonzalez M, Kim E, Hammers H, van Diest PJ, Carducci MA, Kachhap SK. Targeting prostate cancer cell lines with polo-like kinase 1 inhibitors as a single agent and in combination with histone deacetylase inhibitors. FASEB J. 2013 Oct;27(10):4279-93. doi: 10.1096/fj.12-222893. Epub 2013 Jul 24. PubMed PMID: 23884428.

7: Brassesco MS, Pezuk JA, Morales AG, de Oliveira JC, Roberto GM, da Silva GN, Francisco de Oliveira H, Scrideli CA, Tone LG. In vitro targeting of Polo-like kinase 1 in bladder carcinoma: comparative effects of four potent inhibitors. Cancer Biol Ther. 2013 Jul;14(7):648-57. doi: 10.4161/cbt.25087. Epub 2013 May 31. PubMed PMID: 23792639; PubMed Central PMCID: PMC3742494.

8: Fingas CD, Mertens JC, Razumilava N, Sydor S, Bronk SF, Christensen JD, Rizvi SH, Canbay A, Treckmann JW, Paul A, Sirica AE, Gores GJ. Polo-like kinase 2 is a mediator of hedgehog survival signaling in cholangiocarcinoma. Hepatology. 2013 Oct;58(4):1362-74. doi: 10.1002/hep.26484. Epub 2013 Aug 6. PubMed PMID: 23703673; PubMed Central PMCID: PMC3811036.

9: Sanhaji M, Louwen F, Zimmer B, Kreis NN, Roth S, Yuan J. Polo-like kinase 1 inhibitors, mitotic stress and the tumor suppressor p53. Cell Cycle. 2013 May 1;12(9):1340-51. doi: 10.4161/cc.24573. Epub 2013 Apr 10. PubMed PMID: 23574746; PubMed Central PMCID: PMC3674062.

10: Kothari V, Wei I, Shankar S, Kalyana-Sundaram S, Wang L, Ma LW, Vats P, Grasso CS, Robinson DR, Wu YM, Cao X, Simeone DM, Chinnaiyan AM, Kumar-Sinha C. Outlier kinase expression by RNA sequencing as targets for precision therapy. Cancer Discov. 2013 Mar;3(3):280-93. doi: 10.1158/2159-8290.CD-12-0336. Epub 2013 Feb 5. PubMed PMID: 23384775; PubMed Central PMCID: PMC3597439.