BI 2536

目錄號(hào): HY-50698 純度: 99.92%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

BI 2536 是 PLK1 和 BRD4 的雙抑制劑，IC₅₀ 分別為 0.83 和 25 nM。BI-2536 抑制 IFNB (IFN-β，干擾素 β) 基因轉(zhuǎn)錄。

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BI 2536 Chemical Structure

CAS No. : 755038-02-9

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規(guī)格	價(jià)格	是否有貨
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		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

•Mol Cancer. 2023 May 20;22(1):86. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•EMBO J. 2024 Sep 26. [Abstract]
•Biomark Res. 2024 Jun 9;12(1):59. [Abstract]
•Cancer Res. 2022 Feb 15;82(4):681-694. [Abstract]
•Nat Commun. 2018 Oct 15;9(1):4275. [Abstract]

•Nat Commun. 2017 Nov 22;8(1):1701. [Abstract]
•Cancer Res. 2017 Sep 15;77(18):4785-4796. [Abstract]
•Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
•Cell Death Dis. 2016 Dec 1;7(12):e2505. [Abstract]
•Cell Rep. 2024 Oct 8;43(10):114827. [Abstract]
•EMBO Rep. 2023 Jun 9;e56100. [Abstract]
•Biomed Pharmacother. December 2021, 112347.
•EMBO Rep. (2021)e51847.
•J Cell Biol. 2021 Feb 1;220(2):e201911025. [Abstract]
•Elife. 2019 Jan 15;8:e39356. [Abstract]
•Int Immunopharmacol. 2024 Apr 30:133:112145. [Abstract]
•PLoS Genet. 2023 Aug 28;19(8):e1010903. [Abstract]
•Biochem Pharmacol. 2023 May 19;213:115618. [Abstract]
•Pharmaceutics. 2022 Jun 6;14(6):1209. [Abstract]
•iScience. 2022 May 30;25(6):104476. [Abstract]
•J Photochem Photobiol B. 2022 May 20;232:112477. [Abstract]
•Development. 2022 May 15;149(10):dev200351. [Abstract]
•Cells. 2021, 10(8), 1859.
•Mol Cancer Ther. 2018 Apr;17(4):825-837. [Abstract]
•J Photochem Photobiol B. 2017 Jul;172:77-87. [Abstract]
•Sci Rep. 2016 Nov 22;5:37581. [Abstract]
•Oncol Lett. 2024 May 14.
•Cancer Chemother Pharmacol. 2024 Mar 27. [Abstract]
•Oncol Lett. 2022 May;23(5):146. [Abstract]
•Vet Microbiol. 2020 Nov;250:108860. [Abstract]
•PLoS Negl Trop Dis. 2016 Jan 11;10(1):e0004356. [Abstract]
•bioRxiv. 2024 Jul 25.
•bioRxiv. 2023.
•Research Square Preprint. 2021 Jan.
•Department of Physiology, Development and Neuroscience & Trinity College. University of Cambridge. 2018 Aug.
•Patent. US20180235964A1.
•Department of Pathology. University of California. 2016.
•College of Pharmacy. Seoul National University. 2015 Feb.
•J Biomol Screen. 2013 Oct;18(9):1062-71. [Abstract]
•Harvard Medical School LINCS LIBRARY

: 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 相關(guān)產(chǎn)品

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查看 Polo-like Kinase (PLK) 亞型特異性產(chǎn)品:

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PLK1 PLK2 PLK3 PLK4

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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)

細(xì)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]

體外研究
(In Vitro)

超過從 10 nM 開始的 100 倍濃度范圍，BI 2536 導(dǎo)致 HeLa 細(xì)胞以 4N DNA 含量積累，表明 G2 期或有絲分裂中的細(xì)胞周期阻滯。除了 HeLa 細(xì)胞外，BI 2536 還能有效抑制一組 32 種人類癌細(xì)胞系的增殖，這些細(xì)胞系代表不同的器官衍生 (包括乳腺癌、結(jié)腸癌、肺癌、胰腺癌和前列腺癌、黑色素瘤和造血系統(tǒng)癌) 和多種多樣的腫瘤抑制基因或癌基因突變的模式 (包括 RB1、TP53、PTEN 和KRAS 狀態(tài))。該細(xì)胞組的半數(shù)最大有效濃度 (EC₅₀) 值范圍為 2-25 nM，而濃度為 100 nM 的 BI 2536 通常足以誘導(dǎo)完全的有絲分裂停滯。指數(shù)生長的 hTERT-RPE1、人臍靜脈內(nèi)皮細(xì)胞 (HUVEC) 和正常大鼠腎 (NRK) 細(xì)胞的增殖在 12-31 nM 的 EC₅₀ 值范圍內(nèi)被阻斷，表明與將未轉(zhuǎn)化的細(xì)胞循環(huán)至 BI 2536^[3]。

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

體內(nèi)研究
(In Vivo)

BI 2536 (40-50 mg/kg，iv) 在免疫缺陷的 nu/nu 小鼠中阻止人類癌癥異種移植物的生長。每周一次或兩次靜脈注射 40-50 mg/kg BI 2536 的連續(xù)周期被發(fā)現(xiàn)在不同的異種移植模型中非常有效，例如 HCT 116 結(jié)腸癌完全抑制腫瘤，每周兩次時(shí)間表 (處理與每周一次處理的對(duì)照 (T/C) 值為 0.3%，T/C 值為 16%；根據(jù)臨床體征和沒有重大體重變化來判斷，這兩種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 號(hào)

755038-02-9

性狀

固體

顏色

White to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 65 mg/mL (124.60 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

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

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.25 mg/mL (6.23 mM); 澄清溶液

此方案可獲得 ≥ 3.25 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 32.5 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.25 mg/mL (6.23 mM); 澄清溶液

此方案可獲得 ≥ 3.25 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 32.5 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.99 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

方案一

請(qǐng)依序添加每種溶劑： 50% PEG300 50% Saline
Solubility: 25 mg/mL (47.92 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

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

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.95%

選擇批次：

Data Sheet (660 KB) SDS (393 KB)

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

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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

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MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

BI 2536 相關(guān)產(chǎn)品

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摩爾計(jì)算器

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BI 2536 相關(guān)分類

完整儲(chǔ)備液配制表

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BI 2536

Customer Review

BI 2536 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

BI 2536 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Polo-like Kinase (PLK) 亞型特異性產(chǎn)品:

生物活性

實(shí)驗(yàn)參考方法

純度 & 產(chǎn)品資料

參考文獻(xiàn)

BI 2536 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

BI 2536 相關(guān)分類

完整儲(chǔ)備液配制表

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