BI 2536
755038-02-9
99%
2026-07-26
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName BI 2536 Cat No CEI-0295 Description BI 2536 can inhibit PLK1 with IC50 of 0.83 nM. CAS No 755038-02-9 Molecular Weight 521.66 Purity >99% Storage 2 years at -20centigrade Powder Targets PLK1 Molecular Formula C28H39N7O3 Chemical Name (R)-4-(8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide Solubility DMSO 96 mg/mL Water In vitro BI 2536 is a potent and selective inhibitor of Plk1 (Polo-like kinase 1), while Polo-like kinase 1 is characterized extensively to further understanding of mitotic mechanisms and as potential targets for cancer therapy. BI 2536 blocks Plk1 activity fully and instantaneously. BI 2536 inhibited primary human cells (HUVEC) with IC50 of 30 nM. And BI 2536 blocked the cancer cell line HeLa with IC50 of 9 nM. Cells treated with BI 2536 are delayed in prophase but eventually import Cdk1-cyclin B into the nucleus, enter prometaphase, and degrade cyclin A. BI 2536-treated cells lack prophase microtubule asters and thus polymerize mitotic microtubules only after nuclear-envelope breakdown and form monopolar spindles that do not stably attach to kinetochores. BI 2536 potently caused a mitotic arrest and induced apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature. (1) Chronic myeloid leukemia (CML) BI 2536 can inhibit proliferation of imatinib-sensitive and imatinib-resistant CML cells. BI 2536 inhibited leukemic cells, which carries the T315 mutation of BCR/ABL with IC50 values from 1nM to 50 nM. The growth-inhibitory effects of BI 2536 on CML cells were found to be associated with cell cycle arrest and apoptosis. BI 2536 also synergized with imatinib and nilotinib in producing growth inhibition in CML cells. (2) Cardiac fibroblasts BI 2536 had a profound effect on cardiac fibroblast proliferation in vitro and arrested these cells in mitosis with an IC50 of about 43 nM. In vivo BI 2536 inhibited growth of human tumor xenografts in nude mice and induces regression of large tumors. category Inhibitors(c1514) cas_num 755038-02-9 Basic Info-
Product Name:
BI 2536
Other Name:Benzamide,4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-;4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide;(R)-4-[(8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide;BI 2536;BI 2356;BI2536
CAS No.:755038-02-9
Molecular Formula:C28H39N7O3
InChIKeys:InChIKey=XQVVPGYIWAGRNI-JOCHJYFZSA-N
Molecular Weight:521.662
Exact Mass:521.65
EC Number:1308068-626-2
Categories:
Characteristics-
PSA:
103
XLogP3:3.7
Density:1.3±0.1 g/cm3
Refractive Index:1.634
Hazard IdentificationClassification of the substance or mixture
no data available
GHS label elements, including precautionary statements
Pictogram(s) no data available Signal word no data available
Hazard statement(s) no data available
Precautionary statement(s) Prevention no data available
Response no data available
Storage no data available
Disposal no data available
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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