Description Features In vitro In vivo
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Volasertib (BI 6727)

Description Features In vitro In vivo
Product Name
Volasertib (BI 6727)
CAS No.
755038-65-4
Chemical Name
Volasertib (BI 6727)
Synonyms
Volasertib;BI-6727;BI 6727; BI-6727; BI6727;CS-552;CS-1612;Volaserib;Volasertib, >=98%;BI6727 (Volasertib);Volasertib (BI 6727);Volasertib (BI 6727) USP/EP/BP
CBNumber
CB12501403
Molecular Formula
C34H50N8O3
Formula Weight
618.81
MOL File
755038-65-4.mol
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Volasertib (BI 6727) Property

Melting point:
86 - 87*C
Density 
1.26
storage temp. 
-20°
solubility 
Soluble in DMSO (up to at least 25 mg/ml).
pka
14.26±0.40(Predicted)
form 
solid
color 
Off-white
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
CAS DataBase Reference
755038-65-4
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18193
Product name
BI 6727
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
18193
Product name
BI 6727
Purity
≥98%
Packaging
5mg
Price
$142
Updated
2024/03/01
Cayman Chemical
Product number
18193
Product name
BI 6727
Purity
≥98%
Packaging
10mg
Price
$249
Updated
2024/03/01
Cayman Chemical
Product number
18193
Product name
BI 6727
Purity
≥98%
Packaging
25mg
Price
$530
Updated
2024/03/01
TRC
Product number
V575180
Product name
Volasertib
Packaging
5mg
Price
$60
Updated
2021/12/16
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Volasertib (BI 6727) Chemical Properties,Usage,Production

Description

Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6-and 65-fold greater selectivity against Plk2 and Plk3. Phase 3.

Features

A high volume of distribution, indicating good tissue penetration, and a long terminal half-life.

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.

Description

Volasertib (755038-65-4) is an extremely potent and selective inhibitor (IC50’s: Plk1= 0.87 nM, Plk2 = 5 nM, Plk3 = 56 nM) of Polo-like kinase 1, a critical controller of multiple essential steps of mitosis.1?It has shown efficacy in multiple solid xenograft tumors models1?and in clinical studies in patients with acute myeloid leukemia2. Volasertib has also been shown to potently inhibit BRD43?(Kd = 79 nM3, IC50’s bromodomains 1 and 2 of BRD4 = 300 and 770 nM respectively2).

Uses

Volasertib (BI 6727) is a highly potent Polo-like kinase (PLK) inhibitor.

target

Polo-like kinase

References

1) Rudolph?et al.?(2009)?BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity; Clin. Cancer Res.?15?3094 2) Rudolph?et al.?(2015)?Efficacy and Mechanism of Action of Volasertib, a Potent and Selective Inhibitor of Polo-Like Kinases, in Preclinical Models of Acute Myeloid Leukemia; J. Pharmacol. Exp. Ther.?352?579 3) Ciceri?et al.?(2014)?Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol.?10?305

Volasertib (BI 6727) Preparation Products And Raw materials

Raw materials

Preparation Products

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Volasertib (BI 6727) Suppliers

China 127 India 2 United States 17 Global 146
MedBioPharmaceutical Technology Inc
Tel
021-69568360 18916172912
Email
order@med-bio.cn
Country
China
ProdList
8140
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8418
Advantage
55
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9976
Advantage
60
XiaoGan ShenYuan ChemPharm co,ltd
Tel
15527768850
Email
1791901229@qq.com
Country
China
ProdList
8836
Advantage
52
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com (International market)
Country
China
ProdList
1856
Advantage
62
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4727
Advantage
58
Artis Chemistry (Shanghai) Co. Ltd.
Tel
86-21-60936353
Fax
86-21-60936352
Country
China
ProdList
335
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
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View Lastest Price from Volasertib (BI 6727) manufacturers

Wuhan Monad Medicine Tech Co.,LTD
Product
Volasertib 755038-65-4
Price
US $10.00/KG
Min. Order
25Kg/Drum
Purity
99.99%
Supply Ability
20 tons/month
Release date
2021-04-16
Career Henan Chemical Co
Product
Volasertib (BI 6727) 755038-65-4
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
20kg
Release date
2018-08-13

755038-65-4, Volasertib (BI 6727)Related Search:

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