BI 2536
BI 2536 Basic information
- Product Name:
- BI 2536
- Synonyms:
-
- 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
- CAS:
- 755038-02-9
- MF:
- C28H39N7O3
- MW:
- 521.65
- EINECS:
- 1308068-626-2
- Product Categories:
-
- Inhibitors
- API
- Mol File:
- 755038-02-9.mol
BI 2536 Chemical Properties
- 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.
BI 2536 Usage And Synthesis
Description
BI 2536 (755038-02-9) was originally reported as a potent (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM)1?and selective2?Polo-like kinase inhibitor?that caused mitotic arrest and apoptosis induction in various human cancer cell lines.1?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 Plk1.4
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.
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
BI 2536Supplier
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- sales@boylechem.com
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