天天操夜夜操,一超碰,亚洲AV片在线观看,亚洲骚国产精品中文

    ABT-263 (Navitoclax) 是 Bcl-xL、Bcl-2 和 Bcl-w 的抑制劑，Ki 分別≤0.5 nM、≤1 nM 和≤1 nM[1]。

ABT-263 (Navitoclax) 在一些但不是所有類型的衰老細胞中具有衰老作用:Navitoclax 降低衰老的人臍靜脈上皮細胞 (HUVEC)、IMR90 人肺成纖維細胞和鼠胚胎成纖維細胞 (MEF) 的活力[2]。 Navitoclax (1μM ; 60 hours)主要通過抑制Bcl-xL[8]加速細胞凋亡。

ABT-263 (Navitoclax) 在 8 種卵巢癌細胞系中表現(xiàn)出適度的 (IC50=3-8 μM) 單藥效力。 Navitoclax(0.4μM;30h) 增強 Igrov-1 細胞中卡鉑和/或紫杉醇誘導(dǎo)的半胱天冬酶 3/7 的激活[3]。從 vavP-Bcl-2 轉(zhuǎn)基因小鼠的胸腺或 BM 中分離出的多個淋巴亞群對 ABT-263 (Navitoclax)[4] 明顯更敏感。

ABT-263 (Navitoclax)（100 mg/kg/d；p.o；每日一次，持續(xù) 21 天）處理接種 H345 細胞的小鼠模型，觀察到顯著的抗腫瘤功效[6] . Navitoclax 聯(lián)合維奈托克和化療對復(fù)發(fā)/難治性急性淋巴細胞白血病或淋巴細胞淋巴瘤患者具有良好的耐受性，并具有良好的療效[5]。在代表 9 種不同組織學(xué)的 44 個異種移植模型中，ABT-263 (Navitoclax)（100 mg/kg/d；i.g；21 天）證明了針對 PPTP（兒科臨床前測試程序）實體瘤組的有限單一藥劑體內(nèi)活性，但顯示出顯著的ALL 面板中針對異種移植物的活性[7]。

產(chǎn)品性質(zhì)：

Cas No.:923564-51-6

別名:Navitoclax,ABT-263,ABT263,ABT 263

化學(xué)名: (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

Canonical SMILES: CC(CC1)(C)CC(CN2CCN(C3=CC=C(C(NS(C4=CC=C(N[C@@H](CSC5=CC=CC=C5)CCN6CCOCC6)C(S(C(F)(F)F)(=O)=O)=C4)(=O)=O)=O)C=C3)CC2)=C1C7=CC=C(Cl)C=C7

分子式:C47H55ClF3N5O6S3

分子量:974.61

溶解度:≥ 48.7305mg/mL in DMSO

儲存條件:Desiccate at -20°C

注意事項：

為了您的安全和健康，請穿實驗服并戴一次性手套操作。

References:

[1]. Tse C, Shoemaker AR, et,al. ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 2008 May 1;68(9):3421-8. doi: 10.1158/0008-5472.CAN-07-5836. PMID: 18451170.

[2]. Zhu Y, Tchkonia T, et,al.Identification of a novel senolytic agent, navitoclax, targeting the Bcl-2 family of anti-apoptotic factors. Aging Cell. 2016 Jun;15(3):428-35. doi: 10.1111/acel.12445. Epub 2016 Mar 18. PMID: 26711051; PMCID: PMC4854923.

[3]. Stamelos VA, Robinson E, et,al. Navitoclax augments the activity of carboplatin and paclitaxel combinations in ovarian cancer cells. Gynecol Oncol. 2013 Feb;128(2):377-82. doi: 10.1016/j.ygyno.2012.11.019. Epub 2012 Nov 17. PMID: 23168176.

[4]. Mérino D, Khaw SL, et,al. Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells. Blood. 2012 Jun 14;119(24):5807-16. doi: 10.1182/blood-2011-12-400929. Epub 2012 Apr 26. PMID: 22538851; PMCID: PMC3382939.

[5]. Pullarkat VA, Lacayo NJ, et,al.Venetoclax and Navitoclax in Combination with Chemotherapy in Patients with Relapsed or Refractory Acute Lymphoblastic Leukemia and Lymphoblastic Lymphoma. Cancer Discov. 2021 Jun;11(6):1440-1453. doi: 10.1158/2159-8290.CD-20-1465. Epub 2021 Feb 16. PMID: 33593877; PMCID: PMC9533326.

[6]. Shoemaker AR, Mitten MJ, et,al. Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res. 2008 Jun 1;14(11):3268-77. doi: 10.1158/1078-0432.CCR-07-4622. PMID: 18519752.

[7]. Lock R, Carol H, et,al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-9. doi: 10.1002/pbc.21433. PMID: 18085673.

[8].Shi J, Zhou Y, Huang HC, Mitchison TJ. Navitoclax (ABT-263) accelerates apoptosis during drug-induced mitotic arrest by antagonizing Bcl-xL. Cancer Res. 2011 Jul 1;71(13):4518-26. doi: 10.1158/0008-5472.CAN-10-4336. Epub 2011 May 5. PMID: 21546570; PMCID: PMC3129452.