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Dinaciclib

PS-095760,SCH727965

Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂，作用于CDK2， CDK5， CDK1和CDK9，IC50分别为1 nM， 1 nM， 3 nM和4 nM，也抑制胸甘(dThd) DNA摄入。

目录号
EY1089
EY1089
EY1089
EY1089
纯度
99.33%
99.33%
99.33%
99.33%
规格
5 mg
10 mg
50 mg
100 mg
原价
920
1400
4300
6200
售价
920
1400
4300
6200
库存
现货
现货
现货
现货
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  • 生物活性

    Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively. Dinaciclib is also a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells (IC50 = 4 nM). Significantly, complete suppression of Rb phosphorylation is correlated with the onset of apoptosis, as indicated by the appearance of the p85 PARP cleavage product in cells exposed to >6.25 nM. Dinaciclib is active against a broad spectrum of human tumor cell lines.

  • 体外研究

  • 体内研究

    2% DMSO+30% PEG 300+ddH2O

  • 激酶实验

  • 细胞实验

    0 μM-5 μM

  • 动物实验

    8 mg/kg, 16 mg/kg, 32 mg/kg,和 48 mg/kg 腹腔注射

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Parry D, et al. Mol Cancer Ther. 2010, 9(8), 2344-2453.
    [2] Feldmann G, Mishra A, Bisht S, Karikari C, Garrido-Laguna I, Rasheed Z, Ottenhof NA, Dadon T, Alvarez H, Fendrich V, Rajeshkumar NV, Matsui W, Brossart P, Hidalgo M, Bannerji R, Maitra A, Nelkin BD. Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft models. Cancer Biol Ther. 2011 Oct 1;12(7):598-609.
    [3] Fu, Wei et al. The cyclin-dependent kinase inhibitor SCH 727965 (Dinacliclib) induces the apoptosis of osteosarcoma cells. Molecular Cancer Therapeutics (2011), 10(6), 1018-1027.

    分子式
    C21H28N6O2    		 分子量
    396.48    		 CAS号
    779353-01-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >30 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    26 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01650727 Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Drug: Dinaciclib|Biological: Rituximab Merck Sharp & Dohme Corp. Phase 1 2012-10-01 2015-02-09
    NCT01676753 Advanced or Metastatic Breast Cancer|Triple Negative Breast Cancer Drug: Dinaciclib & pembrolizumab treatment Jo Chien|Merck Sharp & Dohme Corp.|University of California, San Francisco Phase 1|Phase 2 2016-06-01 2017-03-15
    NCT02684617 rrCLL|rrMM|rrDLBCL Biological: pembrolizumab|Drug: dinaciclib Merck Sharp & Dohme Corp. Phase 1 2016-03-01 2017-02-10
    NCT01783171 Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unresectable Pancreatic Carcinoma Drug: Akt Inhibitor MK2206|Drug: Dinaciclib|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2013-01-01 2017-01-31
    NCT01624441 Estrogen Receptor Negative|HER2/Neu Negative|Male Breast Carcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma Drug: Dinaciclib|Drug: Epirubicin Hydrochloride|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 1 2012-08-01 2017-01-31
    NCT01434316 BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Solid Neoplasm Drug: Dinaciclib|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Veliparib National Cancer Institute (NCI) Phase 1 2011-11-01 2017-01-31
    NCT01711528 Recurrent Plasma Cell Myeloma Drug: Bortezomib|Drug: Dexamethasone|Drug: Dinaciclib|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 1 2012-12-01 2017-01-31
    NCT01026324 Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma Drug: dinaciclib|Other: pharmacological study|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1|Phase 2 2009-09-01 2016-06-22
    NCT01580228 Chronic Lymphocytic Leukemia (CLL) Drug: Dinaciclib|Drug: Ofatumumab Merck Sharp & Dohme Corp. Phase 3 2012-08-01 2017-02-17
    NCT01515176 Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia Drug: Dinaciclib|Other: Laboratory Biomarker Analysis|Biological: Ofatumumab|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1|Phase 2 2012-01-01 2017-02-07
    NCT00937937 Acral Lentiginous Melanoma|Lentigo Maligna Melanoma|Mucosal Melanoma|Nodular Melanoma|Recurrent Melanoma|Stage IV Skin Melanoma|Superficial Spreading Melanoma Drug: Dinaciclib National Cancer Institute (NCI) Phase 2 2009-07-01 2017-02-02
    NCT01096342 Refractory Multiple Myeloma Drug: dinaciclib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2009-07-01 2014-06-02
    NCT00798213 Leukemia, Myeloid, Acute|Lymphoblastic Leukemia, Acute Drug: SCH 727965|Drug: Gemtuzumab ozogamicin Merck Sharp & Dohme Corp. Phase 2 2009-01-01 2015-02-03
    NCT00871663 Solid Tumors|Lymphoma, Non-Hodgkin|Multiple Myeloma|Leukemia, Lymphocytic, Chronic. B-Cell Drug: SCH 727965 Merck Sharp & Dohme Corp. Phase 1 2006-08-01 2015-04-17
    NCT00871546 Lymphoma, Mantle-Cell|Leukemia, Lymphocytic, Chronic, B-Cell Drug: SCH 727965|Drug: Bortezomib|Biological: Alemtuzumab Merck Sharp & Dohme Corp. Phase 2 2009-03-01 2015-08-06
    NCT00871910 Solid Tumors|Lymphoma, Non-Hodgkin|Multiple Myeloma Drug: SCH 727965|Drug: SCH 727965|Drug: SCH 727965|Drug: SCH 727965|Drug: Aprepitant|Drug: Ondansetron|Drug: Dexamethasone Merck Sharp & Dohme Corp. Phase 1 2006-10-01 2015-06-05
    NCT00732810 Breast Neoplasms|Carcinoma, Non-Small-Cell Lung Drug: SCH 727965|Drug: Capecitabine|Drug: Erlotinib Merck Sharp & Dohme Corp. Phase 2 2008-07-01 2015-08-04

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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