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Signaling Pathway



(BI 6727; BI-6727; BI6727)


Volasertib Chemical Structure

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.

Price and Availability of Volasertib

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Size Price Stock Quantity
10 mM * 1 mL $131 In-stock
5 mg $96 In-stock
10 mg $168 In-stock
50 mg $536 In-stock
100 mg $950 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL €128 In-stock
5 mg €94 In-stock
10 mg €165 In-stock
50 mg €525 In-stock
100 mg €931 In-stock
200 mg Get quote
500 mg Get quote

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Volasertib Data Sheet

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    Purity: 99.11%

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Related Compound Libraries

Inhibitor Kit

Biological Activity of Volasertib

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.
IC50 Value: 0.87 nM
Target: PLK1
in vitro: Like BI2536, BI6727 is an ATP-competitive kinase inhibitor from 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 at concentrations up to 10 μM displays no inhibitory activity against a panel of >50 other kinases. 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, respectively. BI6727 treatment (100 nM) in NCI-H460 cells induces an accumulation of mitotic cells with monopolar spindles and positive staining for histone H3 phosphoserine 10, confirming that cells are arrested early in the M phase, followed by induction of apoptosis. Low nanomolar concentrations of BI6727 display potent inhibitory activity against neuroblastoma (NB) tumor-initiating cells (NB TIC) with EC50 of 21 nM, whereas only micromolar concentrations of BI6727 are cytotoxic for normal pediatric neural stem cells. BI6727 induces growth arrest of Daoy and ONS-76 medulloblastoma cells similar to BI 2536.
in vivo: Administration of BI6727 significantly inhibits the growth of multiple human carcinoma xenografts including HCT116, NCI-H460, and taxane-resistant CXB1 colon carcinoma, accompanied by an increase in the mitotic index as well as an increase in apoptosis. In in vivo studies, BI6727 shows better toxicity and pharmacokinetic profile compared to BI2536.

Protocol (Extracted from published papers and Only for reference)

Cell assay [3] Cancer cell lines were obtained from the American Type Culture Collection or the German National Resource Center for Biological Material and were cultured according to the supplier's instructions. Cell proliferation assays were done by inc

Chemical Information

M.Wt 618.81 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C34H50N8O3
CAS No 755038-65-4
Solvent & Solubility

DMSO ≥22mg/mL Water <1.2mg/mL Ethanol ≥122mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.6160 mL 8.0800 mL 16.1600 mL
5 mM 0.3232 mL 1.6160 mL 3.2320 mL
10 mM 0.1616 mL 0.8080 mL 1.6160 mL

Clinical Information of Volasertib

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Volasertib Boehringer Ingelheim Pharmaceuticals Inc Acute myelogenous leukemia 30-NOV-08 30-SEP-13 Phase 2 15-NOV-13
Boehringer Ingelheim Corp Acute myelogenous leukemia 31-JAN-13 30-APR-16 Phase 3 15-NOV-13
Boehringer Ingelheim Pharmaceuticals Inc Ovary tumor 30-APR-10 31-MAY-13 Phase 2 15-NOV-13
Boehringer Ingelheim Corp Bladder cancer 30-NOV-09 31-DEC-11 Phase 2 07-NOV-13
Boehringer Ingelheim Corp Urinary tract tumor 30-NOV-09 31-DEC-11 Phase 2 07-NOV-13
Boehringer Ingelheim Corp Metastatic non small cell lung cancer 31-MAR-09 30-SEP-12 Phase 2 04-NOV-13

References on Volasertib

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