Cdk4 InhibitorA cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties

Cdk4 Inhibitor (CAS 546102-60-7)

Cdk4 Inhibitor | CAS 546102-60-7 is rated 5.0 out of 5 by 1.
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Synonym: 2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
Application: A cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties
CAS Number: 546102-60-7
Molecular Weight: 404.22
Molecular Formula: C20H10BrN3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cdk4 Inhibitor is a cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties. Acts as a potent, selective, and ATP-competitive inhibitor of Cdk4/cyclin D1 (IC50 = 76 nM). It inhibits the activity of other Cdk's only at much higher concentrations (IC50 = 520 nM and 2.1 μM for Cdk2/cyclin E and Cdc2 (Cdk1)/cyclin B, respectively) and shows little activity towards CaMKII, PKA, or GSK-3b (IC50 ≥ 12.4 μM). Shown to inhibit tumor cells growth (IC50 < 3.0 μM in HCT-116 and NCI-H460 cells) by blocking Rb phosphorylation and inducing G1 cell cycle arrest.


References

Zhu, G., et al. 2003. J. Med. Chem. 46, 2027.

Physical State :
Solid
Solubility :
Soluble in DMSO (1 mg/ml).
Storage :
Store at 4° C
Melting Point :
325° C (Predicted)
Refractive Index :
n20D 1.96 (Predicted)
IC50 :
Cdk4/D1: IC50 = 76 nM; Cdk2/E: IC50 = 520 nM; Cdk1/B: IC50 = 2.1 µM; NCI-H460 : IC50 = 2760 nM (human); HCT-116 : IC50 = 2230 nM (human)
pK Values :
pKa: 10.27
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5330797
SMILES :
C1=CC=C2C(=C1)C3=C4C(=C5C6=C(C=C(C=C6)Br)NC5=C3N2)C(=O)NC4=O

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Certificate of Analysis

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Cdk4 Inhibitor  Product Citations

See how others have used Cdk4 Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 25823926  2015. Oncotarget. 6: 8900-13.

PMID: # 25731732  2015. Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine. 36: 5987-97.

PMID: # 21714634  Sakamoto, K. et al. 2011. J Ocul Pharmacol Ther. 27: 419-425.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Sakamoto et al Sakamoto et al. (PubMed ID 21714634) found that rats treated with CDK4 inhibitor before ischemia reduced death of retinal ganglion cells and reduced mitotic CDK4 activity. -SCBT Publication Review
Date published: 2015-07-19
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