Product Name :
BI-2536 — PLK1 and BRD4 Dual Inhibitor
Description:
BI-2536 is a potent inhibitor of PLK1 (Polo-like kinase 1, IC50 ~0.83 nM) and BRD4 (IC50 ~37 nM). It also inhibits PLK2 and PLK3 with IC50 of 3.5 nM and 9.0 nM, respectively. BI-2536 treatment ranging from 10 nM to 100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, and other Plk1 dependent processes. BI-2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM. It also displaces BRD4 from chromatin and suppresses c-Myc expression. The combination of inhibitory activities on independent kinase and bromodomain oncogenic pathways exemplifies a new strategy for rational single-agent polypharmacological targeting.
CAS:
755038-02-9
Molecular Weight:
521.65
Formula:
C28H39N7O3
Chemical Name:
(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
Smiles :
CC[C@@H]1C(=O)N(C)C2=CN=C(NC3=CC=C(C=C3OC)C(=O)NC3CCN(C)CC3)N=C2N1C1CCCC1
InChiKey:
XQVVPGYIWAGRNI-JOCHJYFZSA-N
InChi :
InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
BI-2536 is a potent inhibitor of PLK1 (Polo-like kinase 1, IC50 ~0.83 nM) and BRD4 (IC50 ~37 nM). It also inhibits PLK2 and PLK3 with IC50 of 3.5 nM and 9.0 nM, respectively. BI-2536 treatment ranging from 10 nM to 100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, and other Plk1 dependent processes. BI-2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM.{{Methylprednisolone} site|{Methylprednisolone} Immunology/Inflammation|{Methylprednisolone} Purity & Documentation|{Methylprednisolone} In Vitro|{Methylprednisolone} manufacturer|{Methylprednisolone} Autophagy} It also displaces BRD4 from chromatin and suppresses c-Myc expression.{{Farletuzumab} site|{Farletuzumab} Antibiotic|{Farletuzumab} Purity & Documentation|{Farletuzumab} Description|{Farletuzumab} supplier|{Farletuzumab} Epigenetics} The combination of inhibitory activities on independent kinase and bromodomain oncogenic pathways exemplifies a new strategy for rational single-agent polypharmacological targeting.PMID:23376608 |Product information|CAS Number: 755038-02-9|Molecular Weight: 521.65|Formula: C28H39N7O3|Chemical Name: (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|Smiles: CC[C@@H]1C(=O)N(C)C2=CN=C(NC3=CC=C(C=C3OC)C(=O)NC3CCN(C)CC3)N=C2N1C1CCCC1|InChiKey: XQVVPGYIWAGRNI-JOCHJYFZSA-N|InChi: InChI=1S/C28H39N7O3/c1-5-22-27(37)34(3)23-17-29-28(32-25(23)35(22)20-8-6-7-9-20)31-21-11-10-18(16-24(21)38-4)26(36)30-19-12-14-33(2)15-13-19/h10-11,16-17,19-20,22H,5-9,12-15H2,1-4H3,(H,30,36)(H,29,31,32)/t22-/m1/s1|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 40 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|BI-2536 was used at 0.1-1 µM in vitro.|In Vivo:|BI-2536 was dosed to mice by IV injection at 50 mg/kg once or twice a week in xenograft models. (Formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl)|References:|Steegmaier M, et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. (2007) Curr Biol. 17(4):316-22.Nappi TC, et al. Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma. (2009) Cancer Res. 69(5):1916-23.Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. (2014) Nat Chem Biol. In press.Products are for research use only. Not for human use.|Documents||