MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。

I-BET151

CAS No. : 1300031-49-5

產(chǎn)品活性：I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC₅₀ of 6.1, 6.3, and 6.6, respectively.

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：Epigenetic Reader Domain

In Vitro: I-BET151 (1 μM; 72 hours) treatment displays the majority of live cells resided in the G₀ phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.
I-BET151 (100 nM; 72 hours) causes a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G₂ phase.

In Vivo: I-BET151 demonstrates low blood clearance in the rat (~20% liver blood flow) and good oral systemic exposure which resulted in good oral bioavailability. High clearance is observed in the dog (~95% liver blood flow). The systemic exposure in the dog is low, resulting in a poor oral bioavailability of 16%. The high blood clearance in dog correlates well with the high intrinsic clearance observed in dog microsomes and hepatocytes, whereas the low intrinsic clearances seen in rat and mouse (mouse IVC 1.6 mL/min/g; CLb 8 mL/min/kg) correlate with lower in vivo blood clearances in these species. Due to the low systemic exposure observed in the dog, I-BET151 is investigated in the mini-pig as a potential second species for toxicological evaluation where it showed low clearance (~32% liver blood flow) and good bioavailability (65%).
I-BET151 (30 mg/kg; i.p.; daily for 21 days)-treats mice has four- to five fold smaller myeloma tumors and a significantly reduces rate of tumor size doubling than vehicle-treated mice.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Reprogramming Compound Library  |  Anti-Blood Cancer Compound Library  |  Heterocyclic Compound Library  |  BRD4 Inhibitor-18  |  ACBI2  |  BI01826025  |  Curcumin  |  GSK6853  |  MI-1  |  GSK 4027  |  ZL0590  |  BRD4 Inhibitor-26  |  Apabetalone  |  PROTAC BRD2/BRD4 degrader-1  |  MS645  |  OF-1  |  I-CBP112  |  BRM/BRG1 ATP Inhibitor-2  |  UMB-32  |  Ziftomenib  |  GSK761  |  KB02-JQ1  |  CD235  |  VZ185  |  BET-IN-6  |  PLK1/BRD4-IN-1  |  MI-136  |  SF2523  |  SNIPER(BRD)-1  |  Anacardic Acid  |  NI-42

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標(biāo)記物  |  寡核苷酸  |  抗體  |  點(diǎn)擊化學(xué)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動(dòng)劑涉及各熱門信號(hào)通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項(xiàng)目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測(cè)分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報(bào)告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級(jí)期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團(tuán)隊(duì)跟蹤新的制藥及生命科學(xué)研究進(jìn)展，為您提供*新的活性化合物；
•   與世界各大制藥公司及*科研機(jī)構(gòu)建立了長(zhǎng)期的合作。