BI6727 (Volasertib)
BI6727 (Volasertib; CAS 755038-65-4) is a selective inhibitor of Polo-like kinases (Plk), primarily targeting Plk1 with an IC50 of 0.87 nM, and showing lower potency towards Plk2 (IC50 = 5 nM) and Plk3 (IC50 = 56 nM). Plk1 regulates the G2/M cell cycle transition and is commonly overexpressed in various tumor types, representing a potential therapeutic target. BI6727 inhibits proliferation across multiple tumor cell lines including colorectal (HCT116, EC50 = 23 nM), lung (NCI-H460, EC50 = 21 nM), melanoma (BRO, EC50 = 11 nM), and hematologic cancer (GRANTA, EC50 = 15 nM). In vivo, BI6727 administration induced apoptosis and reduced tumor growth in mouse HCT116 and NCI-H460 xenograft models.
- 1. Van der Feen DE, Kurakula K, et al. "Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension." Am J Respir Crit Care Med. 2019 May 1. PMID:31042405
- 2. Zheng DW, Xue YQ, et al. "Volasertib suppresses the growth of human hepatocellular carcinoma in vitro and in vivo." Am J Cancer Res. 2016 Nov 1;6(11):2476-2488. PMID:27904765
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 618.83 |
| Cas No. | 755038-65-4 |
| Formula | C34H50N8O3 |
| Synonyms | BI 6727; BI-6727 |
| Solubility | insoluble in H2O; ≥10.31 mg/mL in DMSO; ≥56.1 mg/mL in EtOH |
| Chemical Name | N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide |
| SDF | Download SDF |
| Canonical SMILES | CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Human melanoma A375 and Hs 294T cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
24 h, 10-100 nM |
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Applications |
BI6727 (Volasertib) is a second generation small molecule Plk1 inhibitor and has been reported to be a promising agent for treatment of several cancers. BI6727 (Volasertib) inhibits growth, viability and induces apoptosis of melanoma cells. |
| Clinical experiment [2]: | |
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Animal models |
Patients aged ≥ 18 years with locally advanced or metastatic urothelial cancer |
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Dosage form |
BI6727 (Volasertib) was administered by 2-hour intravenous infusion at a dose of 300 mg once daily on day 1 of 3-week treatment cycles. |
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Application |
BI6727 (Volasertib) has an acceptable safety profile as a second-line treatment for advanced or metastatic urothelial cancer, but only modest antitumor activity for further evaluation as a monotherapy. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Cholewa B D, Ndiaye M A, Huang W, et al. Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo[J]. Cancer Letters, 2017, 385: 179-187. [2]. Stadler W M, Vaughn D J, Sonpavde G, et al. 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[J]. Cancer, 2014, 120(7): 976-982. |
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| Description | BI6727 is a high potent inhibitor of Polo-like kinase with IC50 value of 0.87 nM. | |||||
| Targets | Polo-like kinase | |||||
| IC50 | 0.87 nM | |||||
Quality Control & MSDS
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Chemical structure
Related Biological Data
Related Biological Data
