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Abemaciclib,CDK4/6 抑制剂

Abemaciclib,CDK4/6 抑制剂

规格或纯度: 97%

CAS编号: 1231929-97-7
分子式: C₂₇H₃₂F₂N₈
分子量: 506.59
PubChem编号: 46220502

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货号 (SKU)	包装规格	是否现货
L190223-250mg	250mg	现货
L190223-1g	1g	现货
L190223-5g	5g	现货

查看相关系列

cyclin dependent kinase 4 Inhibitor cyclin dependent kinase 6 Inhibitor

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基本描述

别名

N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-异丙基-1H-苯并咪唑-6-基]-2-嘧啶胺;玻玛西林;阿贝西利

英文别名

LY2835219

规格或纯度

97%

英文名称

Abemaciclib

储存温度

避光,-20°C储存

运输条件

超低温冰袋运输

产品介绍

Abemaciclib highly selective inhibits the complexes CDK4/ cyclin D1 (IC50 =2 nmol/L) and CDK6/cyclin D1 (IC50 =10 nmol/L), with no activity against other CDK/cyclin complexes or cell-cycle-related kinases within the nanomolar ranges, except for inhibition of CDK9 at IC50 at least five times higher. Besides the cell-cycle dependent activity, abemaciclib is able to boost antitumor immunity by potentiating tumor antigen presentation and selectively suppressing proliferation of regulatory T (Treg) cells at the same time. Consistent with its activity against CDK4 and CDK6, abemaciclib inhibits RB phosphorylation and leads to G1 arrest in RB-proficient cell lines. In vitro, treatment with abemaciclib resulted in increased activation of human T cells and upregulated expression of antigen presentation genes in MCF-7 breast cancer cells.

名称和标识符

IUPAC Name	N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine
INCHI	InChI=1S/C27H32F2N8/c1-5-35-8-10-36(11-9-35)16-19-6-7-24(30-14-19)33-27-31-15-22(29)25(34-27)20-12-21(28)26-23(13-20)37(17(2)3)18(4)32-26/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34)
InChi Key	UZWDCWONPYILKI-UHFFFAOYSA-N
Canonical SMILES	CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F
PubChem CID	46220502
分子量	506.59

数据库链接

PubChem CID	46220502
CAS Registry No.	1231929-97-7
ChEMBL Ligand	CHEMBL3301610
RCSB PDB Ligand	6ZV
DrugCentral Ligand	5259

化学和物理性质

溶解性	insoluble in H2O; ≥4.83 mg/mL in DMSO with gentle warming and ultrasonic; ≥6.34 mg/mL in EtOH with gentle warming
敏感性	对光敏感

安全和危险性（GHS）

象形图	Health Hazard
信号词	Danger
危险声明	H373: Causes damage to organs through prolonged or repeated exposure H410: Very toxic to aquatic life with long lasting effects H360: May damage fertility or the unborn child
预防措施声明	P273,P280,P308+P313,P314

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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. Goel S, Wang Q, Watt AC, Tolaney SM, Dillon DA, Li W, Ramm S, Palmer AC, Yuzugullu H, Varadan V et al.. (2016) Overcoming Therapeutic Resistance in HER2-Positive Breast Cancers with CDK4/6 Inhibitors.. Cancer Cell, 29 (3): (255-69). [PMID:26977878]