| Identification | More | [Name]
BI 2536 | [CAS]
755038-02-9 | [Synonyms]
BI 2536
BI-2536(R-)
BI2536/BI-2536
Boehringer PLK-1 inhibitor
BI-2536, BoehringerPLK-1 inhibitor
4-(8-cyclopentyl-7-ethyl-5-Methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylaMino)-3-Methoxy-N-(1-Methylpiperidin-4-yl)benzaMide
(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-[[(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
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)-
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 | [EINECS(EC#)]
1308068-626-2 | [Molecular Formula]
C28H39N7O3 | [MDL Number]
MFCD10565924 | [MOL File]
755038-02-9.mol | [Molecular Weight]
521.662 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
4°C, protect from light | [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 |
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