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Dinaciclib (SCH727965),新型CDK抑制剂, 细胞周期蛋白依赖性激酶 9 抑制剂

新型有效的选择性细胞周期蛋白依赖性激酶(CDK)抑制剂
规格或纯度: ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
D127362-5mg
5mg 现货 Stock Image
D127362-25mg
25mg 现货 Stock Image
D127362-100mg
100mg 现货 Stock Image

基本描述

英文别名 Dinaciclib|779353-01-4|SCH727965|Dinaciclib (SCH727965)|SCH 727965|SCH-727965|MK-7965|(S)-3-(((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)methyl)pyridine 1-oxide|(2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]py
规格或纯度 ≥98%
英文名称 Dinaciclib (SCH727965)
生化机理 Dinaciclib(SCH 727965 ) is a pyrazolo[1,5-a]pyrimidine with potential antineoplastic activity. Dinaciclib(SCH 727965 ) selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9; inhibition of CDK1 and CDK2 may result in cell cycle repression and tumor cell apoptosis.Novel, potent, selective cyclin-dependent kinase (CDK) inhibitor displaying selectivity for CDK1, CDK2, CDK5 and CDK9 (IC 50 values\xa0are 3, 1, 1 and 4 nM respectively). Potent DNA replication inhibitor\xa0that blocks thymidine incorporation in A2780 ova
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Dinaciclib (SCH727965)是CDK抑制剂,对CDK2,CDK5,CDK1和CDK9的IC50分别为1 nM,1 nM,3 nM和4 nM。A novel and potent cyclin-dependent kinase inhibitor for Cdk2, Cdk5, Cdk1, and Cdk9

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 in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation.
A novel and potent cyclin-dependent kinase inhibitor for Cdk2, Cdk5, Cdk1, and Cdk9

产品属性

ALogP 1.9

名称和标识符

IUPAC Name 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol
INCHI InChI=1S/C21H28N6O2/c1-2-17-14-23-27-19(22-13-16-6-5-9-25(29)15-16)12-20(24-21(17)27)26-10-4-3-7-18(26)8-11-28/h5-6,9,12,14-15,18,22,28H,2-4,7-8,10-11,13H2,1H3/t18-/m0/s1
InChi Key PIMQWRZWLQKKBJ-SFHVURJKSA-N
Canonical SMILES CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO
Isomeric SMILES CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCC[C@H]4CCO
PubChem CID 46926350
分子量 396.49

化学和物理性质

溶解性 DMSO: ≥ 56 mg/mL
熔点 107-111°C

安全和危险性(GHS)

象形图
ghs08

Health Hazard

ghs07

Harmful

信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H372: Causes damage to organs through prolonged or repeated exposure
H340: May cause genetic defects
预防措施声明 P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P260,P281,P270,P362+P364,P203,P264+P265,P318,P337+P317,P332+P317,P319

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参考文献

1. Beroukhim R, Mermel CH, Porter D, Wei G, Raychaudhuri S, Donovan J, Barretina J, Boehm JS, Dobson J, Urashima M et al..  (2010)  The landscape of somatic copy-number alteration across human cancers..  Nature,  463  (7283):  (899-905).  [PMID:20164920]
2. Puyol M, Martín A, Dubus P, Mulero F, Pizcueta P, Khan G, Guerra C, Santamaría D, Barbacid M.  (2010)  A synthetic lethal interaction between K-Ras oncogenes and Cdk4 unveils a therapeutic strategy for non-small cell lung carcinoma..  Cancer Cell,  18  (1):  (63-73).  [PMID:20609353]
3. Dean JL, McClendon AK, Hickey TE, Butler LM, Tilley WD, Witkiewicz AK, Knudsen ES.  (2012)  Therapeutic response to CDK4/6 inhibition in breast cancer defined by ex vivo analyses of human tumors..  Cell Cycle,  11  (14):  (2756-61).  [PMID:22767154]
4. Choi YJ, Li X, Hydbring P, Sanda T, Stefano J, Christie AL, Signoretti S, Look AT, Kung AL, von Boehmer H et al..  (2012)  The requirement for cyclin D function in tumor maintenance..  Cancer Cell,  22  (4):  (438-51).  [PMID:23079655]
5. Sawai CM, Freund J, Oh P, Ndiaye-Lobry D, Bretz JC, Strikoudis A, Genesca L, Trimarchi T, Kelliher MA, Clark M et al..  (2012)  Therapeutic targeting of the cyclin D3:CDK4/6 complex in T cell leukemia..  Cancer Cell,  22  (4):  (452-65).  [PMID:23079656]
6. Zhang XH, Cheng Y, Shin JY, Kim JO, Oh JE, Kang JH.  (2013)  A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS..  Cancer Biol Ther,  14  (7):  (597-605).  [PMID:23792647]
7. Martin MP, Olesen SH, Georg GI, Schönbrunn E.  (2013)  Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains..  ACS Chem Biol,  (11):  (2360-5).  [PMID:24007471]