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| 目錄號 | MZ3701-100MG | 售價(jià) | 4188.00元 | ||||||||||||||||||||||||||||||||||
| 規格 | 100mg | 運輸溫度 | 室溫 | ||||||||||||||||||||||||||||||||||
| 其他名稱(chēng) | Veliparib free base; ABT-888; A-861695; NSC 737664; | 保存溫度 | -20ºC干燥保存 | ||||||||||||||||||||||||||||||||||
| CAS號 | 912444-00-9 | 有效期 | 3年 | ||||||||||||||||||||||||||||||||||
| 應用 | PARP1/ PARP2抑制劑 | 訂購數量 |
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產(chǎn)品簡(jiǎn)介: Veliparib (ABT-888) 維利帕尼 點(diǎn)擊丨商城購買(mǎi) 積分領(lǐng)好禮 產(chǎn)品標簽 Veliparib 維利帕尼；ABT-888；PARP1/ PARP2抑制劑；Temozolomide 替莫唑胺；Radiopotentiation輻射增強；chemopotentiation化療增強；CAS：912444-00-9；
產(chǎn)品信息
產(chǎn)品描述 維利帕尼（Veliparib），又稱(chēng)為ABT-888，是一種有效的PARP1和PARP2抑制劑，Ki值分別是5.2nM和2.9nM，對SIRT2沒(méi)有活性。ABT-888具有良好的口服生物活性，能夠穿透血腦屏障，在同源腫瘤模型和異種移植腫瘤模型中增強替莫唑胺（Temozolomide）、鉑類(lèi)、環(huán)磷酰胺和放射效果[1]。ABT-888具有廣譜的化學(xué)和放射增強效應[1-3]。PARP1抑制劑INO-1001和ABT-888明顯減少肌源性緊張度和改善內皮依賴(lài)性舒張，恢復內皮一氧化氮合酶磷酸化和cGMP，以及降低切割PARP1表達。PARP1抑制劑可能用來(lái)克服糖尿病微血管功能障礙[4]。
產(chǎn)品特性 1） CAS NO：912444-00-9 2） 化學(xué)名：1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one 3） 同義名：Veliparib free base; ABT-888; A-861695; NSC 737664; 4） 分子式：C13H16N4O 5） 分子量：244.29 g/mol 6） 純度：>98% 7） 外觀(guān)：白色至類(lèi)白色結晶性固體或粉末 8） 溶解性：溶于DMSO（≥10mg/ml）【“>”：表明溶于標示濃度，但飽和溶解度未知?！?/span>
9）
化學(xué)結構式：
保存與運輸方法 保存：-20oC干燥保存，3年有效。 運輸：常溫運輸。
注意事項 1） 為了讓化合物更好的溶解，可通過(guò)37℃加熱或（和）超聲波水浴中震動(dòng)片刻來(lái)處理。若實(shí)驗所需濃度過(guò)大甚至達產(chǎn)品溶解極限，請添加助溶劑助溶或自行調整濃度。 2） 本品僅用作科研用途，不得用作臨床診斷或治療，不得用于食品或藥品，絕對禁止用在人身上。 3） 為了您的安全和健康，請穿實(shí)驗服并戴一次性手套操作。
儲存液制備
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文獻1，Boerner JL et al. Protein expression of DNA damage repair proteins dictates response to topoisomerase and PARP inhibitors in triple-negative breast cancer. PLoS One. 2015 Mar 16;10(3):e0119614.PMID: 25774912 體外研究（細胞實(shí)驗）： 細胞類(lèi)型（Cell type）：BRCA mutated TNBC cell lines: SUM149, SUM159 and SUM1315; HCC1937 and MDA-MB-231; MX-1; 藥物配制（Preparation）：ABT-888 was dissolved in dimethylsulphoxide (DMSO) to make a stock concentration of 10mM and stored at -20°C. 實(shí)驗方法（Assay）：Exponentially growing cells were seeded in 96-well plates (MX-1: 5,000 per well, all others: 2,000 per well) and the single agent drugs (ABT-888 or CPT-11) were addedin concentrations ranging from 0.01 nM to 100 μM the following day. When the drugs were used in combination, CPT-11 was added to media with a constant ABT-888 concentration of 500nM. Cell proliferation was determined 5 days after continuous exposure to drug by addition of MTT. |
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文獻2，Liu X et al.Potentiation of Temozolomide Cytotoxicity by Poly(ADP)Ribose Polymerase Inhibitor ABT-888 Requires a Conversion of Single-Stranded DNA Damages to Double-Stranded DNA Breaks. Mol Cancer Res. 2008 Oct;6(10):1621-9. PMID: 18922977 體內研究（動(dòng)物模型）： 動(dòng)物模型（Animal Model）：B16F10 melanoma syngeneic model 藥物配制（Preparation）：ABT-888 was delivered in a vehicle containing 0.9% NaCl adjusted to pH 4.0. 實(shí)驗方法（Assay）：B16F10 cells (6×104) were injected s.c. into the flank of female C57BL/6 mice. Mice were injection-order allocated to treatment groups, and therapy was initiated on day 1 following inoculation. ABT-888 was delivered in a vehicle containing 0.9% NaCl adjusted to pH 4.0. Temozolomide was formulated using 0.2% hydroxypropyl methylcellulose.Temozolomide was administered on an oral, qd × 5 schedule on days 6 to 10 at 50 mg/kg/d concurrently with ABT-888 on an oral, bd × 5 schedule at 25, 5, and 1 mg/kg/d.The experiment consists of 10 mice per treatment group; |
參考文獻
[1] Donawho CK et al. ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA- damaging agents in preclinical tumor models. Clin Cancer Res. 2007 May 1;13(9):2728-37.
[2] Shelton JW et al. In vitro and in vivo enhancement of chemoradiation using the oral PARP inhibitor ABT-888 in colorectal cancer cells. Int J Radiat Oncol Biol Phys. 2013 Jul 1;86(3):469-76.
[3] Shunkwiler L et al. Inhibition of Poly(ADP-Ribose) Polymerase Enhances Radiochemosensitivity in Cancers Proficient in DNA Double-Strand Break Repair. Int J Mol Sci. 2013 Feb 8;14(2):3773-85.
[4] Choi SK et al. Poly(ADP-ribose) polymerase 1 inhibition improves coronary arteriole function in type 2 diabetes mellitus. Hypertension. 2012 May;59(5):1060-8.
— —Written/Edited by V. Shallan【版權歸MKBio懋康所有】
上海懋康生物科技有限公司是一家涉足于生命科學(xué)和生物技術(shù)領(lǐng)域研究的試劑、儀器和實(shí)驗室消耗品與實(shí)驗服務(wù)工作，主要從事細胞生物學(xué)、植物學(xué)、分子生物學(xué)、免疫學(xué)、生物化學(xué)、蛋白組學(xué)。生物制藥與診斷試劑研發(fā)生產(chǎn)等領(lǐng)域。 本公司秉承“以人為本，以誠為信、合同守信”的經(jīng)營(yíng)理念。堅持"品質(zhì)保障"的原則為廣大客戶(hù)提供優(yōu)質(zhì)產(chǎn)品。
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