13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯(lián)系人:高小姐
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化學性質：
| 規(guī)格 | 10mM (in 1mL DMSO) 10mg 25mg 50mg |
| CAS | 827022-33-3 |
| 別名 | Palbociclib Isethionate |
| 化學名 | 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;2-hydroxyethanesulfonic acid |
| 分子式 | C24H29N7O2.C2H6O4S |
| 分子量 | 573.66 |
| 溶解度 | ≥ 28.7mg/mL in DMSO |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
IC50: Palbociclib is an orally active, potent and highly selective inhibitor of CDK4 and CDK6, with IC50 values for CDK4/cyclinD1, CDK4/cyclinD3 and CDK6/cyclinD2 of 11, 9 and 15 nmol/l, respectively.
Cyclin-dependent kinases (CDKs) are a family of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. A cyclin-dependent kinase inhibitor (CKI) is a protein that interacts with a cyclin-CDK complex to block kinase activity, usually during G1 or in response to signals from the environment or from damaged DNA. Palbociclib is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.
In vitro: Half-maximal inhibitory concentrations (IC50) of PD-0332991 were determined with cell line proliferation assays. Resutls showed that IC50 values for PD-0332991 ranged from 25.0 nM to 700 nM, and the agent demonstrated G0/G1 cell-cycle arrest, induction of late apoptosis, and blockade of RB phosphorylation. Through genotype and expression data p16, p15 and E2F1 were identified as having significant association between loss and sensitivity to PD-0332991: p16 (p=0.021), p15 (p=0.047), and E2F1 (p=0.041) [1].
In vivo: Oral administration of PD 0332991 to mice bearing the Colo-205 human colon carcinoma produces marked tumor regression. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F. The results indicate that inhibition of Cdk4/6 alone is sufficient to cause tumor regression and a net reduction in tumor burden in some tumors [2].
Clinical trial: In a phase 2 trial reported at the April 2014 annual meeting of the American Association for Cancer Research, the addition of palbociclib to letrozole was shown to significantly slow the progression of advanced cancer (median progression-free survival increased from 10.2 months to 20.2 months), but was not shown to have a statistically significant effect on increasing patients' overall survival times. A potentially confirmatory phase 3 trial, PALOMA-2, has fully enrolled patients. The drug received an accelerated approval from the Food and Drug Administration on February 3, 2015, as a treatment (in combination with letrozole) for patients with estrogen receptor-positive advanced breast cancer (http://en.wikipedia.org/wiki/Palbociclib).
特別提醒：
1. 本產品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。
2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。
原創(chuàng)作者：上海莼試生物技術有限公司
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