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Chemodex
Palbociclib
61
CHF
CHF 61.00
In stock
CDX-P0590-M0055 mgCHF 61.00
CDX-P0590-M02525 mgCHF 251.00
| Product Details | |
|---|---|
| Synonyms | 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one; PD 0332991; PD-332991; PD991; PF 00080665 |
| Product Type | Chemical |
| Properties | |
| Formula |
C24H29N7O2 |
| MW | 447.53 |
| CAS | 571190-30-2 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Light-yellow or off-yellow powder, beige. |
| Solubility | Soluble in DMSO (2mg/ml). |
| Identity | Determined by 1H-NMR. |
| Declaration | Manufactured by Chemodex. |
| Other Product Data |
Click here for Original Manufacturer Product Datasheet |
| InChi Key | AHJRHEGDXFFMBM-UHFFFAOYSA-N |
| Smiles | O=C1C(C(C)=O)=C(C)C(C=NC(NC2=CC=C(N3CCNCC3)C=N2)=N4)=C4N1C5CCCC5 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +20°C |
| Long Term Storage | +20°C |
| Handling Advice | Protect from light and moisture. |
| Use/Stability | Stable for at least 2 years after receipt when stored at RT. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
Palbociclib is a potent and selective inhibitor of CDK4 (IC50=11nM) and CDK6 (IC50=16nM). Displays selectivity for Cdk4/6 over a panel of 36 additional protein kinases. It exhibits selective antiproliferation activity against Rb-positive human breast/colon/lung/leukemia cancer cultures and displays in vivo efficacy against various advanced stage human tumor xenografts in mice. It inhibits phosphorylation of Rb protein and cell cycle progression through G1 in primary 5T33MM cells and sensitized these cells to killing by a proteasome inhibitor (bortezomib) in mouse models. Induces autophagy and senescence in AGS gastric cancer cells. It is a clinically useful breast cancer agent. In addition cell cycle inhibitors have been shown to boost tumor immunogenicity.
Product References
(1) D.W. Fry, et al.; Mol. Cancer Ther. 3, 1427 (2004) | (2) E. Menu, et al.; Cancer Res. 68, 5519 (2008) | (3) R.L. Sutherland & E.A. Musgrove; Breast Cancer Res. 11, 112 (2009) | (4) R.S. Finn, et al.; Breast Cancer Res. 11, R77 (2009) | (5) A. Rocca, et al.; Expert Opin. Pharmacother. 15, 407 (2014) (Review) | (6) J.D. Altenburg & S.S. Farag; Expert Opin. Investig. Drugs 24, 261 (2015) (Review) | (7) A.S. Clark, et al.; JAMA Oncol. 2, 253 (2016) (Review) | (8) C.A. Valenzuela, et al.; Exp. Cell Res. 360, 390 (2017) | (9) S. Goel, et al.; Nature 548, 471 (2017) | (10) M. Schmidt & M. Sebastian; Recent Results Cancer Res. 211, 153 (2018) (Review) | (11) M. Poratti & G. Marzaro; Eur. J. Med. Chem. 172, 143 (2019) (Review)