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530487 StemSelect® PD 0332991 - CAS 827022-32-2 - Calbiochem

A cell-permeable, brain permeant, potent, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC₅₀ = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, HCl, Cdk4/Cdk6 Inhibitor V, PD-0332991, HCl, PF-332991, HCl

Primary Target: Cdk4 & Cdk6
530487
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
827022-32-2C₂₄H₂₉N₇O₂ • HCl

Products

Catalogue NumberPackaging Qty/Pack
5.30487.0001 Glass bottle 5 mg
Description
OverviewA cell-permeable, orally available and brain permeant, non-toxic pyridopyrimidinone compound that acts as a potent, selective, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC50 = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively). Hence, it reduces retinoblastoma protein phosphorylation at Ser780/Ser795 (IC50 = 66 nM in MDA-435 cells) and arrests cell cycle at G1 phase. Acts as a cytostatic agent, but does induce apoptotic cell death when used alone. However, it potentiates the cytotoxicity of dexamethasone (Cat. No. 265005), bortezomib (Cat. No. 504314), and tamoxifen (Cat. No. 579000) in estrogen receptor (ER)-positive cell lines. Exhibits only a trivial inhibitory activity towards Cdk2/E2, Cdk2/A, Cdk1/B and Cdk5/p25 in a 36-kinase panel (IC50 > 10 µM). Improves endoderm differentiation of late G1-human embryonic stem cells expressing Smad2 or Smad3 (~ 750 nM) and further enhances endoderm differentiation into hepatic and pancreatic progenitor cells. Shown to regress the growth of human breast tumor xenografts in murine models (~150 mg/kg, p.o., daily).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number530487
Brand Family Calbiochem®
Synonyms6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, HCl, Cdk4/Cdk6 Inhibitor V, PD-0332991, HCl, PF-332991, HCl
References
ReferencesPauklin, S. and Vallier, L., 2013. Cell 155, 135.
Finn, R.S., et al. 2009. Breast Cancer Res. 11, R17.
Menu, E., et al. 2008. Cancer Res. 68, 5519.
Baughn, L.B., et al. 2006. Cancer Res. 66, 7661.
Fry, D.W., et al. 2004. Mol. Cancer Ther. 3, 1427.
Product Information
CAS number827022-32-2
FormYellow liquid
Hill FormulaC₂₄H₂₉N₇O₂ • HCl
Chemical formulaC₂₄H₂₉N₇O₂ • HCl
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetCdk4 & Cdk6
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Dry Ice Only
Toxicity Standard Handling
Storage ≤ -70°C
Protect from Light Protect from light
Avoid freeze/thaw Avoid freeze/thaw
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.30487.0001 04055977260823

Documentation

StemSelect® PD 0332991 - CAS 827022-32-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Pauklin, S. and Vallier, L., 2013. Cell 155, 135.
Finn, R.S., et al. 2009. Breast Cancer Res. 11, R17.
Menu, E., et al. 2008. Cancer Res. 68, 5519.
Baughn, L.B., et al. 2006. Cancer Res. 66, 7661.
Fry, D.W., et al. 2004. Mol. Cancer Ther. 3, 1427.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision02-May-2014 JSW
Synonyms6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, HCl, Cdk4/Cdk6 Inhibitor V, PD-0332991, HCl, PF-332991, HCl
DescriptionA cell-permeable, orally available and brain permeant, non-toxic pyridopyrimidinone compound that acts as a potent, selective, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC50 = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively). Hence, it reduces retinoblastoma protein phosphorylation at Ser780/Ser795 (IC50 = 66 nM in MDA-435 cells) and arrests cell cycle at G1 phase. Acts as a cytostatic agent, but does induce apoptotic cell death when used alone. However, it potentiates the cytotoxicity of dexamethasone (Cat. No. 265005), bortezomib (Cat. No. 504314), and tamoxifen (Cat. No. 579000) in estrogen receptor (ER)-positive cell lines. Exhibits only a trivial inhibitory activity towards Cdk2/E2, Cdk2/A, Cdk1/B and Cdk5/p25 in a 36-kinase panel (IC50 > 10 µM). Improves endoderm differentiation of late G1-human embryonic stem cells expressing Smad2 or Smad3 (~ 750 nM) and further enhances endoderm differentiation into hepatic and pancreatic progenitor cells. Shown to regress the growth of human breast tumor xenografts in murine models (~150 mg/kg, p.o., daily).
FormYellow liquid
Intert gas (Yes/No) Packaged under inert gas
CAS number827022-32-2
Chemical formulaC₂₄H₂₉N₇O₂ • HCl
Purity≥97% by HPLC
SolubilityH₂O (10 mg/ml)
Storage Protect from light
Avoid freeze/thaw
≤ -70°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesPauklin, S. and Vallier, L., 2013. Cell 155, 135.
Finn, R.S., et al. 2009. Breast Cancer Res. 11, R17.
Menu, E., et al. 2008. Cancer Res. 68, 5519.
Baughn, L.B., et al. 2006. Cancer Res. 66, 7661.
Fry, D.W., et al. 2004. Mol. Cancer Ther. 3, 1427.