PD 0332991 HCl
Pyrido[2,3-d]pyrimidin-7(8H)-one,6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-,monohydrochloride
CAS: 827022-32-2
Molecular Formula: C24H30ClN7O2
PD 0332991 HCl - Names and Identifiers
PD 0332991 HCl - Physico-chemical Properties
| Molecular Formula | C24H30ClN7O2 |
| Molar Mass | 483.9937 |
| Appearance | Yellow liquid |
| Storage Condition | = -70C |
| Use | Palbociclib (PD-0332991) HCl is a highly selective CDK4/6 inhibitor with IC50 of 11 nM/16 nM. It has no inhibitory activity on CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
| In vitro study | PD 0332991 has no inhibitory effect on other protein kinases including EGFR, FGFR, PGFR, IR, etc. When PD 0332991 acts on Cdk4, it is a non-ATP competitive inhibitor. PD 0332991 inhibits MDA-MB-435 breast cancer cells with an IC50 of 66 nM due to decreased phosphorylation of Rb at ser780. PD 0332991 inhibit Thymidine Incorporation into Rb-positive human breast cancer, colon cancer, lung cancer, and leukemia DNA with IC50 values of 4 nM to 0.17 μm. PD 0332991 had no inhibitory effect on Rb negative cells. PD 0332991 acts on MDA-MB-453 breast cancer cells and colon -205 cells to cause cell accumulation in the G1 phase. The PD 0332991 was also effective on myeloma 5T33MM cells, sensitizing the cells to Bortezomib. PD 0332991 inhibits luminalER-positive and her2-enhanced breast cancer cell lines, including MDA-MB-175 ZR-75-30 CAMA-1 MDA-MB-134 HCC-202 UACC-893, among others. In these cell lines, PD 0332991 enhanced the activity of Tamoxifen and Trastuzumab. In MCF7 anti-Tamoxifen cells, PD 0332991 also enhanced the sensitivity of tamoxifen. Recent studies have shown that PD 0332991 can inhibit malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, and KP-MRT-NS, and MRT cell lines have a negative correlation between PD 0332991 sensitivity and p16 expression. |
| In vivo study | Treatment of MDA-MB-435 xenografts with 150 mg/kg PD 0332991 completely inhibited the tumors. PD 0332991 also exhibits broad-spectrum anticancer activity in a variety of human tumor xenografts by removing p-Rb and proliferating Marker Ki-67 from blood vessels and regulating genes that are controlled at the E2F transcriptional level. |
PD 0332991 HCl - Risk and Safety
| HS Code | 29399990 |
PD 0332991 HCl - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.066 ml | 10.331 ml | 20.662 ml |
| 5 mM | 0.413 ml | 2.066 ml | 4.132 ml |
| 10 mM | 0.207 ml | 1.033 ml | 2.066 ml |
| 5 mM | 0.041 ml | 0.207 ml | 0.413 ml |
Last Update：2024-01-02 23:10:35
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Product Name: PD0332991 HCl Visit Supplier Webpage Request for quotation
CAS: 827022-32-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 827022-32-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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