BI 2536
- CAS NO.:755038-02-9
- Empirical Formula: C28H39N7O3
- Molecular Weight: 521.65
- MDL number: MFCD10565924
- EINECS: 1308068-626-2
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:19
What is BI 2536?
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
The Uses of BI 2536
BI 2536 is a PLK1 inhibitor, inducing apoptosis together with micro-tubule-destabilizing drugs in preclinical rhabdomyosarcoma models. Anti-cancer and potent PLK1 inhibitor.
What are the applications of Application
BI 2536 is a Plk inhibitor with efficacy against 32 cancer cell lines
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
Properties of BI 2536
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. |
Safety information for BI 2536
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for BI 2536
New Products
6-Bromo 2-Iodo Indole Pyridine 2,4,6-Tricarboxaldehyde Rimegepant Impurity 3 Ivermectin EP Impurity B Fosfomycin EP impurity D Tubulysin F Tubulysin A Tubulysin D 2,2-diethoxyethanethioamide Diethyl Aluminium Cyanide (1.0 M in Toluene) 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Calcium Sodium Phosphosilicate IH 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine 4,7-Dibromobenzo[c][1,2,5]thiadiazole-5,6-diamine 1-(4-Chlorophenyl)piperidin-2-one 1-(4-Aminophenyl)-3-morpholino-5,6-dihydropyridin-2(1H)-one Diethyl 2,5-di(furan-2-yl)terephthalate 2-Chloro-3-(chloromethyl)pyridine 3,6-Bis(4-iodophenyl)-2,5-dihydropyrrolo[3,4-c]pyrrole-1,4-dione 4-bromo-2,5-difluoro benzoic acid 3-(4-bromo-1H-pyrazol-1-yl)-N,N-dimethylpropanamideRelated products of tetrahydrofuran
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