BI 2536

目录号: HY-50698 纯度: 99.92%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

BI 2536 是 PLK1 和 BRD4 的双抑制剂，IC₅₀ 分别为 0.83 和 25 nM。BI-2536 抑制 IFNB (IFN-β，干扰素 β) 基因转录。

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BI 2536 Chemical Structure

CAS No. : 755038-02-9

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规格	价格	是否有货
5 mg	￥809	In-stock
10 mg	￥1254	In-stock
25 mg	￥1388	In-stock
50 mg	￥2300	In-stock
100 mg	￥4140	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 40 篇科研文献

: BI 2536 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Apr;17(4):825-837. [Abstract]; Effect of Plk1 inhibitor on cell proliferation of TAMR-MCF-7 cells. Effects of BI2536 on Plk1 signaling in TAMR-MCF-7 cells. TAMR-MCF-7 cells are incubated with BI2536 (1, 5 and 10 nM) for 24 h and total cell lysates are subjected to immunoblottings for Plk1, Cdc25c and Cyclin B1.

: BI 2536 purchased from MCE. Usage Cited in: Nat Commun. 2017 Nov 22;8(1):1701. [Abstract]; Cells are transfected and treated with BI 2536 as indicated and were fractionated into cytoplasmic (C) and nuclear (N) fractions analyzed by Western blots. The position of Cdc25 and its phosphorylated forms are indicated by arrows. MEK and Histone H3 are respectively cytoplasmic and nuclear proteins probed as controls.

: BI 2536 purchased from MCE. Usage Cited in: College of Pharmacy. Seoul National University. 2015 Feb.; Plk1 inhibition-mediated down-regulation of cdc25c and up-regulation of cyclin B1 in TAMR-MCF-7. BI 2536 (1, 5 and 10 nM) is treated for either 24 h or 48 h.

BI 2536 相关产品

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PLK1 PLK2 PLK3 PLK4

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively^[1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription^[4].

IC₅₀ & Target^[1]

PLK1

0.83 nM (IC₅₀)

Plk2/Snk

3.5 nM (IC₅₀)

Plk3/Fnk

9 nM (IC₅₀)

BRD4

25 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.05 μM Compound: BI-2536	Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 32631534]
A549	GI₅₀	0.057 μM Compound: BI 2536	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
A549	GI₅₀	57.1 nM Compound: BI 2536	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
HCT-116	IC₅₀	2.03 μM Compound: BI-2536	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability by MTT assay	[PMID: 32631534]
HEK293	IC₅₀	0.3 μM Compound: BI-2536	Inhibition of full-length C-terminal NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay Inhibition of full-length C-terminal NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay	[PMID: 30789735]
HEK293	IC₅₀	0.89 μM Compound: BI-2536	Inhibition of full-length C-terminal NanoLuc-tagged ALK (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay Inhibition of full-length C-terminal NanoLuc-tagged ALK (unknown origin) expressed in human HEK293 cells after 2 hrs by NanoBRET target engagement assay	[PMID: 30789735]
HEK-293T	IC₅₀	0.6 nM Compound: B12536	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
HEK-293T	IC₅₀	1 nM Compound: BI-2536	Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
HeLa	GI₅₀	0.034 μM Compound: BI 2536	Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay	[PMID: 29220793]
HeLa	GI₅₀	34 nM Compound: BI 2536	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
HL-60	IC₅₀	3.42 μM Compound: BI-2536	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
HL-60	IC₅₀	36.5 nM Compound: 1	Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay	[PMID: 26985285]
HRPE	IC₅₀	> 600 nM Compound: BI2536	Antiproliferative activity against human RPE cells expressing C67V mutant PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human RPE cells expressing C67V mutant PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34210138]
HRPE	IC₅₀	27.1 nM Compound: BI2536	Antiproliferative activity against human RPE cells expressing wild-type PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human RPE cells expressing wild-type PLK1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34210138]
Huh-7	GI₅₀	0.028 μM Compound: BI 2536	Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
Huh-7	GI₅₀	28.4 nM Compound: BI 2536	Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
K562	GI₅₀	0.068 μM Compound: BI 2536	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
K562	GI₅₀	60.5 nM Compound: BI 2536	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
MCF7	GI₅₀	0.067 μM Compound: BI 2536	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
MCF7	GI₅₀	67 nM Compound: BI 2536	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
MDA-MB-231	IC₅₀	1 nM Compound: BI-2536	Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MM1.S	IC₅₀	1 nM Compound: BI-2536	Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay	[PMID: 28792760]
MM1.S	IC₅₀	1.2 nM Compound: B12536	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
MV4-11	GI₅₀	0.0152 μM Compound: BI-2536	Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay	[PMID: 26191363]
MV4-11	IC₅₀	0.45 μM Compound: BI-2536	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
NCI-H1975	GI₅₀	0.23 μM Compound: BI 2536	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay	[PMID: 29220793]
NCI-H1975	GI₅₀	130 nM Compound: BI 2536	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31629162]
PC-3	IC₅₀	0.46 μM Compound: BI-2536	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay	[PMID: 32631534]

体外研究
(In Vitro)

超过从 10 nM 开始的 100 倍浓度范围，BI 2536 导致 HeLa 细胞以 4N DNA 含量积累，表明 G2 期或有丝分裂中的细胞周期阻滞。除了 HeLa 细胞外，BI 2536 还能有效抑制一组 32 种人类癌细胞系的增殖，这些细胞系代表不同的器官衍生 (包括乳腺癌、结肠癌、肺癌、胰腺癌和前列腺癌、黑色素瘤和造血系统癌) 和多种多样的肿瘤抑制基因或癌基因突变的模式 (包括 RB1、TP53、PTEN 和KRAS 状态)。该细胞组的半数最大有效浓度 (EC₅₀) 值范围为 2-25 nM，而浓度为 100 nM 的 BI 2536 通常足以诱导完全的有丝分裂停滞。指数生长的 hTERT-RPE1、人脐静脉内皮细胞 (HUVEC) 和正常大鼠肾 (NRK) 细胞的增殖在 12-31 nM 的 EC₅₀ 值范围内被阻断，表明与将未转化的细胞循环至 BI 2536^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BI 2536 (40-50 mg/kg，iv) 在免疫缺陷的 nu/nu 小鼠中阻止人类癌症异种移植物的生长。每周一次或两次静脉注射 40-50 mg/kg BI 2536 的连续周期被发现在不同的异种移植模型中非常有效，例如 HCT 116 结肠癌完全抑制肿瘤，每周两次时间表 (处理与每周一次处理的对照 (T/C) 值为 0.3%，T/C 值为 16%；根据临床体征和没有重大体重变化来判断，这两种方案都具有良好的耐受性^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

521.65

Formula

C₂₈H₃₉N₇O₃

CAS 号

755038-02-9

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 65 mg/mL (124.60 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

0.1 M HCL 中的溶解度 : 25 mg/mL (47.92 mM; ultrasonic and adjust pH to 4 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9170 mL	9.5850 mL	19.1699 mL
5 mM	0.3834 mL	1.9170 mL	3.8340 mL
10 mM	0.1917 mL	0.9585 mL	1.9170 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.25 mg/mL (6.23 mM); 澄清溶液

此方案可获得 ≥ 3.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.25 mg/mL (6.23 mM); 澄清溶液

此方案可获得 ≥ 3.25 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.99 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 25 mg/mL (47.92 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (660 KB) SDS (393 KB)

COA (195 KB) HNMR (213 KB) LCMS (465 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lénárt P, et al. The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15. [Content Brief]

[2]. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6(7):764-9. [Content Brief]

[3]. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322. [Content Brief]

[4]. Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468(3):363-72. [Content Brief]

Cell Assay ^[3]	Cell proliferation assays are performed by incubation in the presence of various concentrations of BI 2536 (10 nM-1 μM) for 72 hr, and cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. Effective concentrations at which cellular growth is inhibited by 50% (EC₅₀) are extrapolated from the dose-response curve fit^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Female BomTac:NMRI-Foxn1nu mice are grafted subcutaneously with HCT 116 colon-carcinoma, NCI-H460, or A549 lung-carcinoma cells by subcutaneous injection, respectively, of 2×10⁶, 1×10⁶, and 1×10⁷ cells into the flank of each mouse. When tumors reached a volume of approximately 50 mm³, animals are pair-matched into treatment and control groups of ten mice each. In regression experiments, treatment is not initiated until the mean tumor volume reached 500 mm³. BI 2536 is injected intravenously into the tail vein at the indicated dose and schedule. The administration volume is 10 mL per kg body weight. Tumor volumes are determined three times a week with a caliper. The results are converted to tumor volume (mm³) by the following formula: length×width²×π/6. The weight of the mice is determined as an indicator of tolerability on the same days. For statistical analysis, the treatment group is compared with the vehicle control group in a one-sided (decreasing) exact Wilcoxon test. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lénárt P, et al. The Small-Molecule Inhibitor BI 2536 Reveals Novel Insights into Mitotic Roles of Polo-like Kinase 1. Curr Biol. 2007 Feb 20;17(4):304-15. [Content Brief] [2]. Chen L, et al. BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536. ACS Med Chem Lett. 2015 May 18;6(7):764-9. [Content Brief] [3]. Steegmaier M, et al. BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo. Current Biology (2007), 17(4), 316-322. [Content Brief] [4]. Malik N, et al. Suppression of IFN β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members. Biochem J. 2015 Jun 15;468(3):363-72. [Content Brief]

BI 2536 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

0.1 M HCL / DMSO	1 mM	1.9170 mL	9.5850 mL	19.1699 mL	47.9249 mL
	5 mM	0.3834 mL	1.9170 mL	3.8340 mL	9.5850 mL
	10 mM	0.1917 mL	0.9585 mL	1.9170 mL	4.7925 mL
	15 mM	0.1278 mL	0.6390 mL	1.2780 mL	3.1950 mL
	20 mM	0.0958 mL	0.4792 mL	0.9585 mL	2.3962 mL
	25 mM	0.0767 mL	0.3834 mL	0.7668 mL	1.9170 mL
	30 mM	0.0639 mL	0.3195 mL	0.6390 mL	1.5975 mL
	40 mM	0.0479 mL	0.2396 mL	0.4792 mL	1.1981 mL
DMSO	50 mM	0.0383 mL	0.1917 mL	0.3834 mL	0.9585 mL
	60 mM	0.0319 mL	0.1597 mL	0.3195 mL	0.7987 mL
	80 mM	0.0240 mL	0.1198 mL	0.2396 mL	0.5991 mL
	100 mM	0.0192 mL	0.0958 mL	0.1917 mL	0.4792 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BI 2536755038-02-9BI2536BI-2536Polo-like Kinase (PLK)Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

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BI 2536

Customer Review

BI 2536 相关抗体

MCE 顾客使用本产品发表的 40 篇科研文献

BI 2536 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

BI 2536 相关抗体:

摩尔计算器

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完整储备液配制表

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