ChemicalBook > CAS DataBase List > BI 2536

BI 2536

Product Name
BI 2536
CAS No.
755038-02-9
Chemical Name
BI 2536
Synonyms
BI 2536;CS-1984;BI-2536(R-);(R)-BI-2536;BI 2536, >=98%;BI2536/BI-2536;BI 2536 USP/EP/BP;BI 2536, 10 mM in DMSO;BI 2536;BI-2536; BI2536;Boehringer PLK-1 inhibitor
CBNumber
CB31562104
Molecular Formula
C28H39N7O3
Formula Weight
521.65
MOL File
755038-02-9.mol
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BI 2536 Property

Density 
1.28
storage temp. 
Keep in dark place,Sealed in dry,Store in freezer, under -20°C
solubility 
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 25 mg/ml)
form 
Yellow powder.
pka
14.09±0.20(Predicted)
color 
Off-white
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
InChIKey
XQVVPGYIWAGRNI-JOCHJYFZSA-N
SMILES
C(NC1CCN(C)CC1)(=O)C1=CC=C(NC2=NC=C3C(=N2)N(C2CCCC2)[C@H](CC)C(=O)N3C)C(OC)=C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

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

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

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17385
Product name
BI 2536
Purity
≥95%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
17385
Product name
BI 2536
Purity
≥95%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
17385
Product name
BI 2536
Purity
≥95%
Packaging
10mg
Price
$178
Updated
2024/03/01
Cayman Chemical
Product number
17385
Product name
BI 2536
Purity
≥95%
Packaging
50mg
Price
$758
Updated
2024/03/01
TRC
Product number
B373470
Product name
BI2536
Packaging
5mg
Price
$105
Updated
2021/12/16
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BI 2536 Chemical Properties,Usage,Production

Description

BI 2536 (755038-02-9) was originally reported as a potent (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) and selective Polo-like kinase inhibitor that caused mitotic arrest and apoptosis induction in various human cancer cell lines. It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells.3?BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1[1-4].

Uses

BI 2536 is a PLK1 inhibitor, inducing apoptosis together with micro-tubule-destabilizing drugs in preclinical rhabdomyosarcoma models. Anti-cancer and potent PLK1 inhibitor.

Biological Activity

BI 2536, an ATP-competitive PLK1 kinase inhibitor, has been shown to inhibit PLK1 enzyme activity at nanomolar concentrations. Studies showed that BI 2536 treatment resulted in cell cycle progression disorder, mitotic catastrophe, growth inhibition and apoptosis in a broad range of cancer cells. Given its potent anti-proliferation activity in various cancer cells and xenograft models, the effect of this compound has been evaluated in clinical studies in several adult cancers.[5].

in vitro

Exceeding a 100-fold concentration range starting at 10 nM, BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either the G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumour suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status). The half-maximal effective concentration (EC50) values in this cell panel ranged from 2-25 nM, whereas a concentration of 100 nM of BI 2536 is typically sufficient for inducing a complete mitotic arrest. The proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells are blocked at EC50values ranging from 12-31 nM, indicating a comparable sensitivity of cycling nontransformed cells to BI 2536.

in vivo

BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. Once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumour suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment; both schedules are well-tolerated, as judged by clinical signs and absence of significant body-weight changes.

target

Plk1

References

1) Steegmaier?et al.?(2007),?BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo; Curr. Biol.,?17?316 2) Davis?et al.?(2011),?Comprehensive analysis of kinase inhibitor selectivity; Nat. Biotechnol.,?29?1046 3) Ciceri?et al.?(2014),?Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol.,?10?305 4) Xiao?et al.?(2016),?Polo-like Kinase-1 Regulates Myc Stabilization and Activates a Feedforward Circuit Promoting Tumor Cell Survival; Mol. Cell,?64?493
[5] Li, Zhiheng et al. “The dual role of BI 2536, a small-molecule inhibitor that targets PLK1, in induction of apoptosis and attenuation of autophagy in neuroblastoma cells.” Journal of Cancer vol. 11,11 3274-3287. 5 Mar. 2020, doi:10.7150/jca.33110

BI 2536 Preparation Products And Raw materials

Raw materials

Preparation Products

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BI 2536 Suppliers

China 146 Germany 1 India 1 The Netherlands 1 United Kingdom 1 United States 24 Global 174
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755038-02-9, BI 2536Related Search:

D-ERYTHRO-SPHINGOSINE Bortezomib Alisertib (MLN8237) PD 0332991 HCl Volasertib (BI 6727) Afatinib Olaparib Selumetinib BML-275 PLX-4720 CX-4945 Fluoxetine hydrochloride Alpelisib (BYL719) Tubastatin A hydrochloride N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide hydrochloride Neratinib Glucagon Receptor Antagonist I BI 2536

  • BI-2536, BoehringerPLK-1 inhibitor
  • 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
  • BI 2536
  • 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)-
  • Boehringer PLK-1 inhibitor
  • BI-2536(R-)
  • BI2536/BI-2536
  • (R)-4-((8-cyclopentyl-7-ethyl-5-Methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)aMino)-3-Methoxy-N-(1-Methylpiperidin-4-yl)benzaMide
  • 4-(8-cyclopentyl-7-ethyl-5-Methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylaMino)-3-Methoxy-N-(1-Methylpiperidin-4-yl)benzaMide
  • BI 2536 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
  • BI 2536, >=98%
  • 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
  • BI 2536;BI-2536; BI2536
  • (R)-BI-2536
  • CS-1984
  • (R)-4-((8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-3-methoxy-
  • BI 2536 USP/EP/BP
  • BI-2536 Plk1 inhibitor potent ATP-competitive
  • BI 2536, 10 mM in DMSO
  • Polo-like Kinase Inhibitor IV
  • 755038-02-9
  • 755038-03-9
  • C28H39N7O3
  • Inhibitors
  • API