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

H3B-6545

CAS No. : 2052130-80-8

產(chǎn)品活性：H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.

研究領(lǐng)域：Vitamin D Related/Nuclear Receptor

作用靶點：Estrogen Receptor/ERR

In Vitro: H3B-6545 is a highly selective small molecule that potently antagonizes wild-type and mutant ERα in biochemical and cell based assays. In vitro comparisons with standard of care and other experimental agents confirm increased cell potency of H3B-6545 under continuous as well as washout treatment conditions. H3B-6545, a member of a novel class of ERα antagonists refer to as selective ER covalent antagonist (SERCA), which inactivates both wild-type and mutant ERα by targeting C530 and enforcing a unique antagonist conformation. H3B-6545 is a first-in-class selective ER covalent antagonist (SERCA). H3B-6545 inhibits ERα^WT activity and growth of ERα^WT -positive breast cancer lines. H3B-6545 potently inhibits ERα^WT activity and suppresses proliferation of ERα^WT -positive breast cancer lines. With GI₅₀s of 0.3-0.4, 1.0, 0.5, 5.2, and 0.2 nM for MCF7, HCC1428, BT483, T47D and CAMA-1 cell lines.

In Vivo: In vivo, once daily oral dosing of H3B-6545 shows potent activity and superior efficacy to fulvestrant in the MCF-7 xenograft model with maximal antitumor activity at doses >10x below the maximum tolerated dose in mice. In addition, H3B-6545 shows superior antitumor activity to Tamoxifen and Fulvestrant in patient derived xenograft models of estrogen receptor positive breast cancer including models carrying ERα mutations in rat and monkeys, H3B-6545 is well tolerated across a broad dose range and at exposures that significantly exceed those required for efficacy in mouse xenograft models.

相關(guān)產(chǎn)品：Estradiol hemihydrate  |  OP-1074  |  GSK-4716  |  LSD1/ER-IN-1  |  Avobenzone  |  Cholesterol-¹³C₂  |  Cholesterol-¹⁸O  |  Diethylstilbestrol  |  ERB-196  |  FLTX1  |  Raloxifene hydrochloride  |  Tamoxifen  |  Estradiol-d₂-1  |  Bazedoxifene acetate  |  FSHR agonist 1  |  Estrone sulfate sodium  |  GNE-502  |  β-Estradiol 17-acetate  |  Enclomiphene  |  AhR modulator-1  |  PAC  |  α-Zearalenol  |  SNIPER(ER)-87  |  ERRα antagonist-2  |  Estradiol-d₂  |  Cholesterol-d₇  |  (Rac)-Hexestrol-d₄  |  Cholesterol-d  |  (E)-4-Hydroxytamoxifen  |  Dihydroresveratrol

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,、激動劑涉及各熱門信號通路及疾病領(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)等科研項目,；
•   提供虛擬篩選,，離子通道篩選，代謝組學(xué)分析檢測分析,，藥物篩選等專業(yè)技術(shù)服務(wù),；
•   設(shè)有專業(yè)的實驗中心和嚴(yán)格的質(zhì)控、驗證體系,；
•   提供 LC/MS,、NMR、HPLC,、手性分析,、元素分析等各項質(zhì)檢報告，確保產(chǎn)品的高純度,、高品質(zhì),；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果,；
•   專業(yè)團隊跟蹤最新的制藥及生命科學(xué)研究進展,，為您提供*新的活性化合物；
•   與世界各大制藥公司及著名科研機構(gòu)建立了長期的合作,。