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Merck

SML4229

BI 2536

≥98% (HPLC), powder, Plk1 inhibitor

Synonym(s):

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, (R)-4-[(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, BI-2536,Polo-like Kinase Inhibitor IV

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About This Item

Empirical Formula (Hill Notation):
C28H39N7O3
CAS Number:
Molecular Weight:
521.65
MDL number:
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(C4CCCC4)[C@@H]5CC)=NC=C3N(C)C5=O)C(OC)=C2

Application

BI 2536 may be used in targeting polo-like kinase 1 (PLK1) in cancer therapy; and studying its role in neuroblastoma.

Biochem/physiol Actions

BI 2536 is an ATP-competitive, potent and selective polo-like kinase 1 (Plk1) inhibitor (Plk1/2/3 IC50 = 0.83/3.5/9.0 nM; [ATP] = 7.5 µM) that induces mitotic arrest and apoptosis in human cancer cultures (EC50 <100 nM among 32 different cancer lines) and suppresses human cancer xenografts tumor growth in nude mice in vivo (50-60 mg/kg i.v. twice weekly on two consecutive days; HCT116 and NCI-H460).


Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



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