2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. ERα degrader-2

ERα degrader-2 是一种选择性雌激素受体降解剂 (SERD)，与 ERα (IC50=17.1 nM) 有较强的结合亲和力，具有较好的降解效果(EC50=0.3 nM)。ERα degrader-2 具有良好的药代动力学特性和优良的成药性质，可用于HER 阳性乳腺癌研究。

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ERα degrader-2

ERα degrader-2 Chemical Structure

CAS No. : 2235396-63-9

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ERα degrader-2 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

查看所有亚型
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER+ breast cancer research[1].

IC50 & Target[1]

ERα

4.6 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
ES-2 IC50
17.1 nM
Compound: D24
Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay
Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay
[PMID: 34056898]
MCF7 IC50
0.27 nM
Compound: D24
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay
[PMID: 34056898]
体外研究
(In Vitro)

ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells[1].

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

ERα degrader-2 相关抗体:
体内研究
(In Vivo)

ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice[1].
ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%[1].

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

Animal Model: MCF-7 human breast cancer xenograft model in nude mice[1]
Dosage: 2 mg/kg; 6 mg/kg
Administration: Oral administration; 2-6 mg/kg; QD; 21 days
Result: Exhibited in vivo efficacy in breast cancer xenograft model.
分子量

492.53

Formula

C29H27F3N2O2
CAS 号
性状

固体

颜色

Brown to reddish brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

ERα degrader-2 相关分类

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:

ERα degrader-22235396-63-9ERα degrader2ERα degrader 2Estrogen Receptor/ERRSERDdegradeMCF-7breast cancerERαHER2+Inhibitorinhibitorinhibit

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}); drag.addEventListener("touchstart",function(ev){ downMove(drag, ev); }) } var dragGeneral = document.querySelector("#loginProGeneral"); var dragLogin = document.querySelector("#loginProLogin"); dragMoves(dragGeneral); dragMoves(dragLogin); }); // var initStopn = 0; // var targetTop = 537; // var targetTopDiv = 0; // var loginDivheight = 430; // isCnProdetail = true; // $('html,body').animate({scrollTop:0},1000); //$(".zhuce").offset().top; // function prodetailLogin() { // var stopn = $(window).scrollTop(); // var stopn2 = $(window).scrollTop() - initStopn; // var promise = $("#main_nav").offset().top; // var winheight= ($(window).height()); // var promisepro = 716; // // // // if (stopn >= promise) { // $('.pro_mask').css("top","88px"); // } // else { // $('.pro_mask').css("top","120px"); // } // // if (winheight < promisepro) { // if (stopn2 > 0) { // if (targetTop > 368) { // targetTop = targetTop - stopn2 <= 368 ? 368 : targetTop - stopn2; // } // } // } else { // if (stopn2 < 0) { // targetTop = targetTop - stopn2 >= 537 ? 537 : targetTop - stopn2; // } // loginDivheight = 430; // $('.pro_login').removeClass('divlogoverflow'); // } // // if (targetTop <= 368) { // let h1 = 650 - winheight; // let new_loginDivheight = h1 >= 0 ? 430 - h1 : 430 ; // $('.pro_login').height(new_loginDivheight); // let c_h = loginDivheight - new_loginDivheight; // targetTop = targetTop - c_h / 2; // loginDivheight = new_loginDivheight; // if (new_loginDivheight < 430) { // $('.pro_login').addClass('divlogoverflow'); // } else { // $('.pro_login').removeClass('divlogoverflow'); // } // // } // // $('.pro_login').css("top", targetTop + "px"); // initStopn = $(window).scrollTop(); // } var sel_array = $('[name="pro_cart_mg_num"]'); var mg_array = $('[name="pro_cart_mg"]'); var dw_sel_array = $('[name="pro_cart_dw_num"]'); var dw_array = $('[name="pro_cart_dw"]'); var eta_showStockType = "1"; var eta_infringementType = "0"; function updateProETA(){ var isChange = false; var isPrepare = false; var isETA = false; // var sel_num = $(currentE).val(); // if (parseInt(sh_stock_num) < parseInt(sel_num)) { // $('#pro_detail_eta').show(); // $('#pro_detail_eta').html(getEtaCnMessage()); // } else { // $('#pro_detail_eta').hide(); // $('#pro_detail_eta').html(""); // } var delivery = ''; dw_sel_array.each(function(index,domEle) { var option_dw = $(dw_array.eq(index)).val().split(";"); var dw_sh_stock_num = option_dw[6]; var dw_us_stock_num = option_dw[7]; var dw_select_num = $(domEle).val(); if (parseInt(dw_sh_stock_num) < parseInt(dw_select_num)) { isETA = true; if (dw_us_stock_num == 9527) { isChange = true; } if (dw_us_stock_num == 99999) { isPrepare = true; } delivery = $(domEle).closest('tr').find('.pro_price_3').text() return false; } }); //alert('isDW:'+isDW); sel_array.each(function(index,domEle){ var select_num = $(domEle).val(); var option_mg = $(mg_array.eq(index)).val().split(";"); var sh_stock_num = option_mg[6]; var us_stock_num = option_mg[7]; var eta_message = ''; if (parseInt(sh_stock_num) < parseInt(select_num)) { isETA = true; if (us_stock_num == 9527) { isChange = true; } if (us_stock_num == 99999) { isPrepare = true; } delivery = $(domEle).closest('tr').find('.pro_price_3').text() return false; } }); // 20200519 wdf if (isETA == true) { if (isPrepare || isChange) { $('#pro_detail_eta').html("预计 " + delivery + " 发货"); } else { var catNo = "HY-132194"; changeCnEtaMessage(isChange); //$('#pro_detail_eta').show(); $('#pro_detail_eta').html(getEtaCnMessage(catNo, isChange)); } } else { //$('#pro_detail_eta').hide(); $('#pro_detail_eta').html(""); } } function qtyChange(){ updateProETA(); } // Product Isoform by WDF 20180508 $(function () { fnSetIC50Style(); fnIsoformWidth(); proRelatedImgCN(); //normalSalineDisplacement(); }); // Isoform width function fnIsoformWidth(){ var isoformProList = $(".isoform-pro-list"); var isoformProListLen = isoformProList.length; for(var i = 0; i < isoformProListLen; i++){ var isoformProSpan = isoformProList.eq(i).find("span"); var isoformProSpanLen = isoformProSpan.length; if(isoformProSpanLen>4) { isoformProSpan.parent().css({"width":"100%"}); isoformProSpan.css({"width":"auto"}); } else { isoformProSpan.parent().css({"width":(isoformProSpanLen/4*100)+"%" }); isoformProSpan.css({"width":(1/isoformProSpanLen*100)+"%" }); } } } /* * Target&IC50 Table => 原理 * 1. 计算每个格子的宽度，如果格子的总宽度 <= iContainerW(固定行宽)，则一行显示; 否则多行显示 * 2. 多行的情况: 列数 = iContainerW/最宽单元格的列宽(取整); 列宽 = iContainerW/列数 * 3. 如果一行中, IC50值全是空，那么这一行 IC50 全隐藏，Isoform 垂直居中对齐 */ function fnSetIC50Style(){ var oContainer = $("#pro-ic50-tbl"); var iContainerW = 827; var spanLen = oContainer.find("span").length; var tdLen = spanLen/2; // 单元格总数 var spanArr = []; var spanTotalW = 0; var spanwMax = 0; // span 相加总长度 var lastW = 0; if(tdLen > 1){ for(var i = 0; i < tdLen; i++){ var spanW = [oContainer.find("td").eq(i).find("span").eq(0).outerWidth(),oContainer.find("td").eq(i).find("span").eq(1).outerWidth()].max(); spanArr.push(spanW); spanTotalW += spanW; if(i==tdLen-1){ lastW = oContainer.find("td").eq(i).find("span").eq(0).outerWidth(); } } } spanwMax = spanArr.max(); // console.log("spanwMax= " + spanwMax); // console.log("spanArr=" +spanArr); // 如果 spanwMax > iContainerW 分行; 否则, 一行显示 if(spanTotalW <= iContainerW){ oContainer.find("td").addClass("ic50-td0"); oContainer.find("td:last-child").css({"width": (iContainerW-lastW)+"px"}); // 最后一列宽度 oContainer.find(".ic50-td0").wrapAll(""); }else { var trtdNum = parseInt(iContainerW / spanwMax); // 每一行的列数 var tdWidth = iContainerW/trtdNum; //列宽 var trLen = spanLen/2/trtdNum; // 总行数 var lastTrNum = spanLen/2%trtdNum; //最后一行的个数 var lastColspan = trtdNum+1-lastTrNum; // 最后一行需要合并的单元格数 for (var j = 0; j < tdLen; j++) { for (var k = 0; k < trLen; k++) { if (parseInt(j / trtdNum) == k) { oContainer.find("td").eq(j).addClass("ic50-td" + k); } } } oContainer.find("td").css({"width": tdWidth + "px"}); // 设置列宽 oContainer.find("td:last-child").attr({"colspan": lastColspan}); //最后一行合并的单元格数量 oContainer.find("td:last-child").css({"width": lastColspan*tdWidth+"px"}); // 最后一列宽度 // tr 分组 for (var k = 0; k < trLen; k++) { oContainer.find(".ic50-td" + k).wrapAll(""); } } oContainer.find("td.ic50-td0 > p:first-child").css({"border-top":"0"}); // 第一行 p 的上border 是0 // 如果一行中 IC50 全是空，则这一行隐藏 var iTrLength = oContainer.find("tr>tr").length; var str = []; var tdLength = 0; console.log("tr="+iTrLength); for(var a = 0; a < iTrLength; a++){ tdLength = oContainer.find("tr>tr").eq(a).find("td").length; for(var b = 0; b < tdLength; b++ ){ var aa = oContainer.find("tr>tr").eq(a).find("td").eq(b).find("p").eq(1).text().replace(/\,|(^\s*)|(\s*$)/g, ""); str[a] += aa; } console.log("str[a]="+str[a]); if(str[a] == "undefined" || str[a] == "" || str[a] == null){ for(var b = 0; b < tdLength; b++ ){ oContainer.find("tr>tr").eq(a).find("td").eq(b).find("p").eq(1).css({"display":"none"}); oContainer.find("tr>tr").eq(a).find("td").eq(b).find("p").eq(0).css({"padding":"0"}); oContainer.find("tr>tr").eq(a).find("td").eq(b).find("p").eq(0).find("span").css({"padding":"8px 18px 6px"}); } } } } //最小值 Array.prototype.min = function() { var min = this[0]; var len = this.length; for (var i = 1; i < len; i++){ if (this[i] < min){ min = this[i]; } } return min; } //最大值 Array.prototype.max = function() { var max = this[0]; var len = this.length; for (var i = 1; i < len; i++){ if (this[i] > max) { max = this[i]; } } return max; } Number.prototype.toFloor = function (num) { return Math.floor(this * Math.pow(10, num)) / Math.pow(10, num); }; // end Product Isoform by WDF 20180203 //0){ return false; } else{ var count=$("#iqDetail_productCount").val().trim(); var amountUnit=$('#amountUnit option:selected').text(); $("#pro_num_p").html(count +" "+amountUnit); $(".form_submit_loading").show(); $(".btn_inquiry_submit").addClass("form_btn_submit_send") .removeClass("btn_inquiry_submit"); $("#btn_inquiry_submit").attr({"disabled":"disabled"}); $("#amountUnit").removeAttr("disabled"); $.ajax({ url:"mce_productDetail!inquiry.shtml", cache: false, data:$("#InquiryForm").serialize(), type:"POST", error: function(data) { $("#notice_titie").html("Uh-oh!"); $("#notice_content").html("It appears that we were unable to send an email to "+$("#cmInqriry_addrEmail1").val().trim()+". 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} else { coa_txt = coa_txt + "LCMS ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-LCMS-link', arrPdf[i].objName, 'LCMS', catalogNo, lot_batch); pdf_array.push(pdf_obj); } }else if(arrPdf[i].objFile=="IR"){ if (isShowPT) { coa_txt = coa_txt + "IR ("+arrPdf[i].objSize+" KB)"; } else { coa_txt = coa_txt + "IR ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-IR-link', arrPdf[i].objName, 'IR', catalogNo, lot_batch); pdf_array.push(pdf_obj); } }else if(arrPdf[i].objFile=="GC"){ if (isShowPT) { coa_txt = coa_txt + "GC ("+arrPdf[i].objSize+" KB)"; } else { coa_txt = coa_txt + "GC ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-GC-link', arrPdf[i].objName, 'GC', catalogNo, lot_batch); pdf_array.push(pdf_obj); } }else if(arrPdf[i].objFile=="OR"){ if (isShowPT) { coa_txt = coa_txt + "OR ("+arrPdf[i].objSize+" KB)"; } else { coa_txt = coa_txt + "OR ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-OR-link', arrPdf[i].objName, 'OR', catalogNo, lot_batch); pdf_array.push(pdf_obj); } }else if(arrPdf[i].objFile=="SDS-PAGE"){ if (isShowPT) { coa_txt = coa_txt + "SDS-PAGE ("+arrPdf[i].objSize+" KB)"; } else { coa_txt = coa_txt + "SDS-PAGE ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-SDS-PAGE-link', arrPdf[i].objName, 'SDS-PAGE', catalogNo, lot_batch); pdf_array.push(pdf_obj); } }else if(arrPdf[i].objFile=="Other Report"){ if (isShowPT) { coa_txt = coa_txt + "Other Report ("+arrPdf[i].objSize+" KB)"; } else { coa_txt = coa_txt + "Other Report ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-Other-Report-link', arrPdf[i].objName, 'Other Report', catalogNo, lot_batch); pdf_array.push(pdf_obj); } }else if(arrPdf[i].objFile=="SEC-HPLC"){ if (isShowPT) { coa_txt = coa_txt + "SEC-HPLC ("+arrPdf[i].objSize+" KB)"; } else { coa_txt = coa_txt + "SEC-HPLC ("+arrPdf[i].objSize+" KB)"; var pdf_obj = new $.PdfObj('J-SEC-HPLC-link', arrPdf[i].objName, 'SEC-HPLC', catalogNo, lot_batch); pdf_array.push(pdf_obj); } } }else{ if(arrPdf[i].objFile=="Purity"){ batch_txt += "纯度： " + arrPdf[i].objName ; } else if (arrPdf[i].objFile=="Assay") { batch_txt += "含量： " + arrPdf[i].objName; } else{ batch_txt += "ee.: " + arrPdf[i].objName ; } } } //pdf_batch.innerHTML = batch_txt; //pdf_coa.innerHTML = coa_txt; $("#productDetailBatch_pdf_batch").html(batch_txt); $("#productDetailBatch_pdf_coa").html(coa_txt); } } if (pdf_array.length>0) { $.each(pdf_array, function(index, pdfobjTemp){ //console.log(pdfobjTemp.pdfname); $("#" + pdfobjTemp.pdfid).click(function () { pagePdfObj = pdfobjTemp; pagePdfObj.proName = `ERα degrader-2`; $("#J-HNMR-form .title").html("Request for " + pagePdfObj.pdftype + " Report"); $("#J-HNMR-form #lotNo").val(pagePdfObj.lotNo); modalOpen("#J-HNMR-form"); getUserBaseMessage(); }); }); } } }); } function Gettext(obj){ var txt=obj.options[obj.options.selectedIndex].text; return txt; } cart_sart(); //]]> function findClinicalsByCatalogNo(){ var catalogNo = "HY-132194"; $.ajax({ url:'mce_productDetail!findClinicalsByCatalogNo.shtml?mathdom='+Math.random(), type: 'post', cache:false, data:{'pro_catalogNo':catalogNo}, dataType: 'json', success:function(data){ var str_head = "" + "" + "NCT Number" + "Sponsor" + "Condition" + "Start Date" + "Phase" + "" + "" + ""; var str_foot = ""; var str_content = ""; $.each(data, function(i, item) { if (i==3) { //alert(i+","+item.phase); str_content += " "; } str_content += "" + item.nctNumber + ""; str_content += "" + item.sponsorCollaberators + ""; str_content += "
" + item.activeCondition + "
"; str_content += "" + item.startDate + ""; str_content += "" + item.phase + ""; }); $('#clinical_seo').html(str_head + str_content + str_foot); proClinicalStyle(); } }) } $("#datasheet_url").show(); $("#datasheet_footer_url").show(); $("#datasheet_span").show(); $("#sds_url").show(); $("#sds_footer_url").show(); $("#sds_span").show(); function checkUrl(c_url,type_id) { /*$.ajax({ url:'mce_productDetail!chenkUrlStatus.shtml?mathdom='+Math.random(), type: 'post', cache:false, data:{'curl':c_url}, dataType: 'json', success:function(data){ if (data.checkUrl == "success") { $("#" + type_id + "_url").show(); $("#" + type_id + "_footer_url").show(); $("#" + type_id + "_span").show(); } } })*/ $.ajax({ url: c_url, type: 'get', cache: false, dataType: 'jsonp', processData: false, complete: function(response) { if (response.status == 200) { $("#" + type_id + "_url").show(); $("#" + type_id + "_footer_url").show(); $("#" + type_id + "_span").show(); } }, error: function(data) {} }); } $(function(){ ChangerProductPdf($("#pdf_batch_no option:selected").val()); fnCPDRelated('#J-cpd-related-lib'); //fnCPDRelated('#J-cpd-related-mol'); //findRelatedProArray(); var pmsOutSessionId = $.cookie('pms-out-init'); console.log(pmsOutSessionId) //遮罩层屏蔽 if (pmsOutSessionId != "" && pmsOutSessionId !=null && pmsOutSessionId != undefined){ $("#loginProLogin").hide(); $("#loginProGeneral").hide(); $("#main").removeClass("gray-text");//遮罩层 $("#detail_price_pro").removeClass("is-disabled");//按钮控制 // // $("#loginProGeneral").hide(); // $("#loginProMask").removeClass("pro_mask"); } }); (function($, h, c) { var a = $([]), e = $.resize = $.extend($.resize, {}), i, k = "setTimeout", j = "resize", d = j + "-special-event", b = "delay", f = "throttleWindow"; e[b] = 350; e[f] = true; $.event.special[j] = { setup : function() { if (!e[f] && this[k]) { return false } var l = $(this); a = a.add(l); $.data(this, d, { w : l.width(), h : l.height() }); if (a.length === 1) { g() } }, teardown : function() { if (!e[f] && this[k]) { return false } var l = $(this); a = a.not(l); l.removeData(d); if (!a.length) { clearTimeout(i) } }, add : function(l) { if (!e[f] && this[k]) { return false } var n; function m(s, o, p) { var q = $(this), r = $.data(this, d); r.w = o !== c ? o : q.width(); r.h = p !== c ? p : q.height(); n.apply(this, arguments) } if ($.isFunction(l)) { n = l; return m } else { n = l.handler; l.handler = m } } }; function g() { i = h[k](function() { a.each(function() { var n = $(this), m = n.width(), l = n.height(), o = $ .data(this, d); if (m !== o.w || l !== o.h) { n.trigger(j, [ o.w = m, o.h = l ]) } }); g() }, e[b]) } })(jQuery, this); $('#loginProLogin').on('mousedown', function() { $('#loginProLogin').css('cursor','grab') }); $('#loginProLogin').on('mouseup', function() { $('#loginProLogin').css('cursor','move') }); $('#loginProGeneral').on('mousedown', function() { $('#loginProGeneral').css('cursor','grab') }); $('#loginProGeneral').on('mouseup', function() { $('#loginProGeneral').css('cursor','move') });