産品簡介:
Veliparib
(ABT-888) 維利帕尼
點擊丨商城(chéng)購買 積分領好禮
産品标簽
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;
産品信息
産品名稱
|
産品編号
|
規格
|
價格(元)
|
Veliparib (ABT-888) 維利帕尼
|
MZ3701-10MG
|
10mg
|
868
|
Veliparib (ABT-888) 維利帕尼
|
MZ3701-50MG
|
50mg
|
2428
|
Veliparib (ABT-888) 維利帕尼
|
MZ3701-100MG
|
100mg
|
4188
|
産品描述
維利帕尼(Veliparib),又(yòu)稱為(wèi)ABT-888,是一(yī)種有效的PARP1和PARP2抑制劑,Ki值分别是5.2nM和2.9nM,對SIRT2沒有活性。ABT-888具有良好的口服生(shēng)物(wù)活性,能(néng)夠穿透血腦(nǎo)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、環磷酰胺和放(fàng)射效果[1]。ABT-888具有廣譜的化學和放(fàng)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内皮依賴性舒張,恢複内皮一(yī)氧化氮合酶磷酸化和cGMP,以及降低(dī)切割PARP1表達。PARP1抑制劑可能(néng)用來克服糖尿病微血管功能(néng)障礙[4]。
産品特性
1) CAS NO:912444-00-9
2) 化學名: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:白(bái)色至類白(bái)色結晶性固體或粉末
8) 溶解性:溶于DMSO(≥10mg/ml)【“>”:表明溶于标示濃度,但飽和溶解度未知。】
9)
化學結構式:
保存與運輸方法
保存:-20ºC幹燥保存,3年(nián)有效。
運輸:常溫運輸。
注意事(shì)項
1)
為(wèi)了讓化合物(wù)更好的溶解,可通(tōng)過37℃加熱或(和)超聲波水(shuǐ)浴中震動片刻來處理。若實驗所需濃度過大甚至達産品溶解極限,請添加助溶劑助溶或自(zì)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(shàng)。
3)
為(wèi)了您的安全和健康,請穿實驗服并戴一(yī)次性手套操作。
儲存液制備
質量
溶劑體積
濃度
|
1mg
|
5mg
|
10mg
|
1mM
|
4.0935 mL
|
20.4675 mL
|
40.9350 mL
|
5mM
|
0.8187 mL
|
4.0935 mL
|
8.1870 mL
|
10mM
|
0.4093 mL
|
2.0467 mL
|
4.0935 mL
|
使用方法【源自(zì)文獻,僅作參考】
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(細胞實驗):
細胞類型(Cell type):BRCA mutated TNBC cell lines: SUM149,
SUM159 and SUM1315; HCC1937 and MDA-MB-231; MX-1;
藥物(wù)配制(Preparation):ABT-888 was dissolved
in dimethylsulphoxide (DMSO) to make a stock concentration of 10mM and stored
at -20°C.
實驗方法(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.
|
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
體内研究(動物(wù)模型):
動物(wù)模型(Animal Model):B16F10 melanoma syngeneic model
藥物(wù)配制(Preparation):ABT-888
was delivered in a vehicle containing 0.9% NaCl adjusted to pH 4.0.
實驗方法(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】
上海夢澤生物科技有限公司是一(yī)家涉足于生(shēng)命科學和生(shēng)物(wù)技(jì)術(shù)領域研究的試劑、儀器(qì)和實驗室消耗品與實驗服務工(gōng)作,主要從(cóng)事(shì)細胞生(shēng)物(wù)學、植物(wù)學、分子生(shēng)物(wù)學、免疫學、生(shēng)物(wù)化學、蛋白(bái)組學。生(shēng)物(wù)制藥與診斷試劑研發生(shēng)産等領域。 本公司秉承“以人為(wèi)本,以誠為(wèi)信、合同守信”的經營理念。堅持"品質保障"的原則為(wèi)廣大客戶提供優質産品。
|