LEE011 hydrochloride - CAS 1211443-80-9
Catalog number: 1211443-80-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H31ClN8O
Molecular Weight:
471.0
COA:
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Targets:
CDK
Description:
CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.Treatment with LEE011 significantly reduced proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis at nanomolar concentrations (mean IC50 = 307 ± 68 nmol/L in sensitive lines). LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. Responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay.
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Purity:
>98%
Related CAS:
1211441-98-3 (Free base); 1374639-75-4 (succinate)
Appearance:
Solid powder
Synonyms:
7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide hydrochloride; Ribociclib hydrochloride; LEE011; LEE-011 LEE 011
MSDS:
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InChIKey:
JZRSIQPIKASMEV-UHFFFAOYSA-N
InChI:
1S/C23H30N8O.ClH/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30;/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1H
Canonical SMILES:
O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C.[H]Cl
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CAS 1211443-80-9 LEE011 hydrochloride

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