Veliparib (ABT-888)

For research use only. Not for use in humans.

目录号：S1004 别名： NSC 737664 中文名称：维利帕尼

CAS No. 912444-00-9

Veliparib (ABT-888, NSC 737664)是一种有效的PARP1和PARP2抑制剂，无细胞试验中K_i分别为5.2 nM和2.9 nM，对SIRT2没有活性。Veliparib 可增加自噬和凋亡。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1277.12	现货
10mg	RMB 973.01	现货
25mg	RMB 1859.13	现货
50mg	RMB 3010.72	现货
100mg	RMB 5053.23	现货
200mg	RMB 8108.1	现货
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客户使用Selleck生产的Veliparib (ABT-888)发表文献176篇：

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产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述

特性

ABT-888增强常见癌症疗法的效果，比如放射疗法和烷基化剂。

靶点

PARP2 ^[1] (Cell-free assay)	PARP1 ^[1] (Cell-free assay)
2.9 nM(Ki)	5.2 nM(Ki)

体外研究

ABT-888有效抑制PARP，作用于PARP-1和PARP-2时K_i值分别为5.2和2.9 nM。ABT-888降低肺癌H460细胞中克隆基因的存活率，且抑制DNA修复。^[1]ABT-888抑制C41细胞，EC50为2 nM。^[2] ABT-888和放射物联用减少肿瘤血管的形成。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
C41	MV;LbY5ie2ViQYPzZZk>		M4nkXVMxKG2rbh?=		NEjhSWdKdmirYnn0bY9vKG:oIGDBVnAyKHerdHigSWM2OCCxZjCwMlAxOiEQvF2=	MlPVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OEi3OlAoRjF7OEi4O\|YxRC:jPh?=
Jurkat	NEnjdXRMcW6jc3WgRZN{[Xl?		M1rISVk3KGh?	MVjEUXNQ	MnfZTY5pcWKrdHnvckBw\iCSQWLQNUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gZ4VtdCC4aXHibYxqfHlid3n0bEBGSzVyIH;mJFMh\|ryP	NH\SR2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{i1NFE6QSd-MkO4OVAyQTl:L3G+
Capan1	NV[zR4FNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MUm3NkBp	M1fmTmROW09?	NXzmUVlUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBDWkODMjDn[Y5mKG23dHH0[YQhcHWvYX6gR4Fx[W5zIHPlcIx{KHerdHigTWM2OCCxZjCzPU44KM7:TR?=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN7OEO4N{c,OjR\|OUizPFM9N2F-
DT40	Ml;1R5l1d3SxeHnjJGF{e2G7		M1nkSVczKGh?	NGfVO3FFVVOR	MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmla3XuJGJTS0F{LXTl[olkcWWwdDDEWFQxKGOnbHzz	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl{MkW4O{c,OjR7MkK1PFc9N2F-
ML-1	M3GyPWFxd3C2b4TpZ{BCe3OjeR?=	NVHZRnVDOi53IN88US=>	M1zweFI1KGh?	NX;GRWhKTE2VTx?=	NH\DflRUgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=>	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh7NUGzOUc,OjR6OUWxN\|U9N2F-
HCT-116	MX;LbY5ie2ViQYPzZZk>	NVqwcYJDOC53IN88US=>	NXLle\|BPOjRiaB?=		M1HMSnBCWlBiYXP0bZZqfHliZHXjdoVie2W\|	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3NEKxN{c,OjNyNUSyNVM9N2F-
UM-SCC1	NXnyUHpQS3m2b4TvfIlkKEG\|c3H5	NXjoUVZvOTBizszN	M3z2VFI1KGh?		NEKxSIVT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=>	NYf0XGpSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NVI3OjBpPkKxPVEzPjJyPD;hQi=>
FaDu	NUHXZ3hCS3m2b4TvfIlkKEG\|c3H5	NFr6RYwyOCEQvF2=	NUi3WGZiOjRiaB?=		MofrVoVlfWOnczD0bIUh[2WubDD2bYFjcWyrdIm=	M3i5clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUGyOlIxLz5{MUmxNlYzODxxYU6=
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HAL-01	M2faSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NV;TU49GUUN3ME25Mlg5PjJizszN	MlXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
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MOLT-13	M1HoT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MX\JR\|UxRTJ7LkO4NVQh\|ryP	M{OyblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
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KU812	M1XZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NYfYWYpRUUN3ME2zNk4{PjR{IN88US=>	Ml\PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
COLO-684	Mn[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M1X5WGlEPTB;M{OuN\|U6QSEQvF2=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
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JVM-3	NIjEVJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NIjCcFJKSzVyPUO1MlU5PjhizszN	M2e1WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
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JVM-2	MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVnjT4tQUUN3ME20Nk46OjB5IN88US=>	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
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MDA-MB-361	Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVnXNYk3UUN3ME20N{45PDF2IN88US=>	NEHtZmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK\|5USU6JRWK8M4E,
BALL-1	NWfYVW5TT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M{XINGlEPTB;NEOuPVU{OiEQvF2=	NYiyPXBoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB4OEexM{c,W0GQR1XSQE9iRg>?
T98G	M2P2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFf1NG5KSzVyPUS0Mlg2OTdizszN	M{LKSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFUxPjh5MT:nQnNCVkeHUkyvZV4>
Mo-T	NV;iVJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NEX5dm5KSzVyPUS1MlY{QDlizszN	NUDUPYZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB4OEexM{c,W0GQR1XSQE9iRg>?
MHH-PREB-1	NFTPdpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MmO0TWM2OD12NT63OVg2KM7:TR?=	NFzie3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK\|5USU6JRWK8M4E,
ALL-PO	NH3lPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MULJR\|UxRTR5LkO3PVEh\|ryP	MnLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVA3QDdzLze+V2FPT0WUPD;hQi=>
NCI-H510A	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MlTnTWM2OD12Nz65NFM1KM7:TR?=	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1NFY5PzFxJ{7TRW5ITVJ:L3G+
ML-2	NHfWV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MVHJR\|UxRTR7Lke4OVYh\|ryP	NGHOepI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODZ6N{GvK\|5USU6JRWK8M4E,

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38; PubMed: 22678161 Breast Cancer Res Treat Effects of AG-014699, AZD-2281, ABT-888, or BSI-201 on the phosphorylation status of Stat3, Akt, ERK, and p38 in MDA-MB-468, MDA-MB-231, and Cal-51 cells after 72 h of treatment	22678161
Immunofluorescence	HuR; PubMed: 28687616 Cancer Res Immunofluorescent images of HuR (green) in MIA PaCa-2 cells treated with PARPi for 12hr. Nuclei were stained with DAPI. Magnification 40X. BRCA1; PubMed: 21917757 Int J Oncol Effects of ABT-888 and/or bortezomib on BRCA1 and RAD51 foci formation. BRCA1 and RAD1 foci induced by ABT-888 were completely resolved in cells cotreated with bortezomib. Image acquisition was performed with an epifluorescence microscope (BX51; Olympus) and multispectral color camera (Nuance FX; CRi) with a 60× or 100× magnification lens and oil immersion.	28687616 21917757
Growth inhibition assay	Cell viability (TNBC cell lines); PubMed: 27880910 Cell Rep BRCA-proficient TNBC cell lines were treated with veliparib in the absence and presence of dinaciclib, demonstrating reduced IC50 values in the presence of dinaciclib. Cell viability (melanoma cells); PubMed: 29956724 Int J Oncol Dose-dependent inhibitory effect of ABT-888 on melanoma cell proliferation. Human melanoma cell lines were exposed to diluents (control; CTRL) or increasing concentrations of ABT-888 for 72 h and their viability was assessed by MTT assay. Absorbance was detected at 540 nm with a microplate reader and data were expressed as a percentage of the CTRL. Data are the means ± SD of 3 experiments performed in triplicate. Statistical significance was calculated against the CTRL (P<0.05; *P<0.01).	27880910 29956724

体内研究

ABT-888推迟NCI-H460 移植瘤模型的肿瘤生长。ABT-888在B16F10 和9L 移植瘤模型中抑制PARP，从而增强temozolomide的抗癌活性。^[1]ABT-888和其他细胞毒素药剂联用作用于MX-1移植瘤模型时显示出强抗癌效力。^[2]在A375和 Colo829移植瘤模型中按肿瘤大小，每千克分别加3和12.5 mg ABT-888，可以看到肿瘤内95%以上PAR被抑制。^[4]

激酶实验：^[1]	- 合并体外PARP实验: 在含有50 mM Tris (pH 为8.0), 1 mM DTT,和 4 mM MgCl₂的缓冲溶液中进行酶活性测定。PARP反应包含1.5 μM [³H]-NAD⁺ (1.6 μCi/mmol), 200 nM 生物素组蛋白 H1, 200 nM slDNA,及1 nM PARP-1或4 nM PARP-2酶。在加有100 μL 反应液的 96孔板上进行SPA检测。在50 μL含有PARP和DNA的2×酶液混合物中加入50 μL 2×NAD⁺基底混合物，反应开始。加入150 μL 1.5 mM 苯甲酰胺反应停止。170uL反应终止液转移到链霉亲和素包被的闪熔镀层上，温育1小时，用微型板块闪烁计数器计数。
细胞实验：^[2]	- 合并 Cell lines: C41细胞 Concentrations: 10 μM 左右 Incubation Time: 0.5小时 Method: 在96孔板上用ABT-888处理C41细胞0.5小时。用1 mM H₂O₂破坏DNA10分钟，PARP被激活。用冰冻的PBS冲洗细胞，然后用预冷的甲醇/丙酮（按7:3比例混合）在−20^oC下固定10 分钟。风干后，用PBS再溶解，然后用溶有5%脱脂奶粉的PBS- Tween封闭液(0.05%)在室温下阻断0.5小时。细胞和PAR抗体按1：50比例在封闭液中室温下温育1小时，然后用PBS-Tween-20冲洗5分钟，然后加入荧光素-5(6)-异硫氰酸酯 (FITC)-联用的二抗和1μg/mL DAPI封闭液中室温下温育1小时。PBS-Tween-20冲洗5分钟后，用荧光微型版计数器分析数据。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 携带NCI-H460, H460, B16F10和9L移植瘤的C57BL/6鼠 Dosages: 25或3.125 mg/kg Administration: 口服处理 (Only for Reference)

参考文献

[4] Kinders RJ, et al, Clin Cancer Res, 2008, 14(21), 6877-6885.

- 合并

溶解度 (25°C)

体外	DMSO	17 mg/mL (69.58 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 0.5% methylcellulose+0.2% Tween 80	5 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Veliparib (ABT-888) SDF

分子量	244.29
化学式	C₁₃H₁₆N₄O
CAS号	912444-00-9
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	NSC 737664

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03044795	Withdrawn	Drug: Veliparib	Cancer	University Medical Center Groningen\|AbbVie\|Dutch Cancer Society	November 2019	Phase 2
NCT02723864	Active not recruiting	Drug: Veliparib + VX-970 + Cisplatin	Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	August 9 2017	Phase 1
NCT02483104	Completed	Drug: veliparib\|Drug: carboplatin\|Drug: paclitaxel	Ovarian Cancer	AbbVie	July 2015	Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

选择性强的PARP抑制剂

AG-14361 : PARP1-selective, K_i<5 nM.
选择性强的PARP抑制剂

UPF 1069 : PARP2-selective, IC50=0.3 μM.
活性最高的PARP抑制剂

MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.
用于临床的PARP抑制剂

Iniparib (BSI-201) : Phase III for solid tumors.
最新的PARP抑制剂

BMN 673 : Novel PARP inhibitor with IC50 of 0.58 nM. Also a potent inhibitor of PARP-2, but does not inhibit PARG and highly sensitive to PTEN mutation.

研究领域

产品类型

定制您的化合物库

Veliparib (ABT-888)

客户使用Selleck生产的Veliparib (ABT-888)发表文献176篇：

产品安全说明书

PARP抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Veliparib (ABT-888) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

相关PARP产品