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StemSelect PD 0332991，5MG，5304870001，Sigma

销售价： ¥ 1386.04 / 件

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订货号： 0BL5604

品牌型号： Sigma 5304870001

货期：询货期

最小订货量： 1件

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商品介绍
规格参数
包装参数

产品介绍 Product Description

General description

A 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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Cdk4 & Cdk6
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Pauklin, S. and Vallier, L., 2013. Cell155, 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

技术参数 Specifications

assay	≥97% (HPLC)
Quality Level	100
form	liquid
manufacturer/tradename	Calbiochem^®
storage condition	OK to freeze,avoid repeated freeze/thaw cycles,protect from light
color	yellow
solubility	water: 10 mg/mL
storage temp.	−70°C
SMILES string	Cl.N5(CCNCC5)c1cnc(cc1)Nc2nc3[n]([c](c(c(c3cn2)C)C(=O)C)=O)C4CCCC4
InChI	1S/C24H29N7O2.ClH/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32;/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29);1H
InChI key	STEQOHNDWONVIF-UHFFFAOYSA-N

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