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BIIB021

別名: CNF2024

BIIB021 (CNF2024)是一種口服有效的，全部人工合成的，小分子HSP90抑制劑，Ki和EC50分別為1.7 nM和38 nM。Phase 2.

BIIB021 Chemical Structure

BIIB021 Chemical Structure

CAS: 848695-25-0

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
5mg 737.1 現(xiàn)貨
25mg 2211.3 現(xiàn)貨
50mg 3333.33 現(xiàn)貨
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BIIB021相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

HSP (HSP90) Signaling Pathways

HSP (HSP90)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
NCI-H295 Cytotoxicity assay 120 mg/kg 5 days Cytotoxicity against human NCI-H295 cells overexpressing PGP xenografted in athymic mouse assessed as inhibition of tumor growth at 120 mg/kg, po qd for 5 days per week for 4 weeks 22938030
HeLa Function assay 10 uM 6 hrs Inhibition of HSP90 in human HeLa cells assessed as induction of chk1 degradation at 10 uM after 6 hrs by Western blot method 28816449
HeLa Function assay 10 uM 6 hrs Inhibition of HSP90 in human HeLa cells assessed as induction of Akt degradation at 10 uM after 6 hrs by Western blot method 28816449
HeLa Function assay 10 uM 6 hrs Inhibition of HSP90 in human HeLa cells assessed as induction of HSP70 protein expression at 10 uM after 6 hrs by Western blot method 28816449
PC3 Function assay 10 uM 6 hrs Inhibition of HSP90 in human PC3 cells assessed as induction of chk1 degradation at 10 uM after 6 hrs by Western blot method 28816449
PC3 Function assay 10 uM 6 hrs Inhibition of HSP90 in human PC3 cells assessed as induction of Akt degradation at 10 uM after 6 hrs by Western blot method 28816449
PC3 Function assay 10 uM 6 hrs Inhibition of HSP90 in human PC3 cells assessed as induction of HSP70 protein expression at 10 uM after 6 hrs by Western blot method 28816449
HL60 Function assay 1 uM 24 hrs Inhibition of HSP90 in human HL60 cells assessed as induction of HSP70 expression at 1 uM after 24 hrs by Western blot analysis 29567459
HL60 Function assay 1 uM 24 hrs Inhibition of HSP90 in human HL60 cells assessed as downregulation of phosphorylated Akt expression at 1 uM after 24 hrs by Western blot analysis 29567459
HL60 Function assay 1 uM 24 hrs Inhibition of HSP90 in human HL60 cells assessed as downregulation of phosphorylated STAT3 expression at 1 uM after 24 hrs by Western blot analysis 29567459
HL60 Function assay 1 uM 24 hrs Inhibition of HDAC in human HL60 cells assessed as upregulation of acetyl-alpha-tubulin levels at 1 uM after 24 hrs by Western blot analysis 29567459
HL60 Function assay 1 uM 24 hrs Inhibition of HDAC in human HL60 cells assessed as upregulation of acetylated histone H3 levels at 1 uM after 24 hrs by Western blot analysis 29567459
Sf9 Function assay 3 hrs Binding affinity to human N-terminal polyHis-tagged HSP90alpha (D9 to E236) alpha-helix conformation expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay, Ki=0.002μM 24332488
Sf9 Function assay 3 hrs Binding affinity to human N-terminal polyHis-tagged HSP90beta (D9 to E236) expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay, Ki=0.004μM 24332488
NCI-H1299 Function assay 12 hrs Reduction in oxygen consumption rate in human NCI-H1299 cells incubated for 12 hrs 25383915
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.15μM 29567459
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay, GI50=0.33μM 29567459
NCI-H1975 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H1975 cells after 48 hrs by sulforhodamine B assay, GI50=0.38μM 29567459
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by sulforhodamine B assay, GI50=0.59μM 29567459
MCF7 Function assay Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2, EC50=0.038μM 22938030
BT474 Function assay Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells, IC50=0.14μM 20608738
MCF7 Function assay Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells, IC50=0.038μM 20055425
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50=0.31μM 31663736
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生物活性

產(chǎn)品描述 BIIB021 (CNF2024)是一種口服有效的，全部人工合成的，小分子HSP90抑制劑，Ki和EC50分別為1.7 nM和38 nM。Phase 2.
特性 BIIB021是全人工合成的口服Hsp90 抑制劑。
靶點(diǎn)
HSP90 [1]
(Cell-free assay)
1.7 nM(Ki)
體外研究(In Vitro)
體外研究活性 BIIB021 結(jié)合到Hsp90的ATP結(jié)合袋中, 干涉Hsp90伴侶功能, 導(dǎo)致客戶蛋白降解和腫瘤生長(zhǎng)受抑制。BIIB021抑制腫瘤細(xì)胞 (BT474, MCF-7, N87, HT29, H1650, H1299, H69和H82) 增殖， IC50為0.06-0.31 μM。BIIB021誘導(dǎo)Hsp90客戶蛋白包括HER-2, AKT, 和Raf-1的降解，以及 正向調(diào)節(jié)Hsp70 和Hsp27。[1] BIIB021 抑制Hodgkin's 淋巴癌細(xì)胞(KM-H2, L428, L540, L540cy, L591, L1236 和DEV) ，IC50 為0.24-0.8 μM。BIIB021 作用于健康個(gè)體的淋巴細(xì)胞時(shí)活性低。BIIB021 抑制NF-κB 活性。BIIB021 誘導(dǎo)Hodgkin's 淋巴癌細(xì)胞中激活 NK細(xì)胞受體NKG2D配體的表達(dá)，導(dǎo)致對(duì)NK細(xì)胞調(diào)節(jié)的死亡敏感性上升。[2] 在體外，BIIB021 增強(qiáng)HNSCCA 細(xì)胞系 (UM11B和JHU12)的放射敏感性，伴隨關(guān)鍵放射反應(yīng)蛋白的表達(dá)下降, 增強(qiáng)凋亡細(xì)胞和增強(qiáng)G2期捕獲。[3]在體內(nèi)外，與17-AAG 相比，作用于腎上腺皮質(zhì)癌H295R,BIIB021更有效。BIIB021的細(xì)胞毒性不受NQO1或Bcl-2 過量表達(dá)缺失影響, 分子損傷與17-AAG降低細(xì)胞殺傷力有關(guān)。[4] BIIB021作用于抗17-AAG細(xì)胞系(NIH-H69,MES SA Dx5,NCI-ADR-RES, Nalm6等等)也有效。[5]
激酶實(shí)驗(yàn) Hsp90結(jié)合實(shí)驗(yàn)
用于熒光偏振競(jìng)爭(zhēng)測(cè)量, FITC-geldanamycin 探針 (20 nM) 和2 mM TCEP 在室溫下 進(jìn)行3 小時(shí), 然后等分置于-80oC儲(chǔ)存。 重組人類Hsp90α (0.8 nM) 和降低的 FITC-geldanamycin (2 nM) 在 含有實(shí)驗(yàn)buffer的96孔板上 在室溫下溫育3 小時(shí)，實(shí)驗(yàn)buffer包含20 mM HEPES (pH 為7.4), 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 2 mM DTT, 0.1 mg/mL BGG,和0.1% (v/v) CHAPS。預(yù)溫育后，加入溶于100% DMSO的BIIB021 ，最終濃度為0.2 nM 到10 μM (最終體積為100 μL, 2% DMSO)。反應(yīng)在室溫下進(jìn)行16小時(shí)，在485和535 nm處測(cè)定熒光值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 BT474, MCF-7, N87, HT29, H1650, H1299, H69和H82細(xì)胞
濃度 3到1×103 nM
孵育時(shí)間 5 天
方法 使用修改的四唑鎓鹽法測(cè)定IC50值。腫瘤細(xì)胞加到96孔板上繁殖 24小時(shí)，然后加入BIIB021。對(duì)照組加入DMSO (0.03-0.003%)。吩嗪硫酸甲酯(儲(chǔ)存濃度為1 mg/mL) 和3-(4,5-二甲基噻唑-2-基)-5-(3-羧甲羥苯基)-2-(4-磺苯基)-2氫-四唑, 內(nèi)鹽 (儲(chǔ)存濃度為2 mg/mL) 按1:20混合，加到96孔板的每孔中，溫育。3-(4,5-二甲基噻唑-2-基)-5-(3-羧甲羥苯基)-2-(4-磺苯基)-2氫-四唑, 內(nèi)鹽的降低， 導(dǎo)致可溶性甲臢分泌到培養(yǎng)基中。溫育4小時(shí), 在490納米處使用分光光度計(jì)測(cè)量甲臢。使用SOFTmaxPRO軟件獲得數(shù)據(jù), 100% 生存力定義為用DMSO處理的細(xì)胞A490，用 3-(4,5-二甲基噻唑-2-基)-5-(3-羧甲羥苯基)-2-(4-磺苯基)-2氫-四唑, 內(nèi)鹽(用DMSO處理細(xì)胞的平均A490 為0.03-0.003%)染色通過A490 值計(jì)算每個(gè)樣本存活百分?jǐn)?shù)，計(jì)算按如下:存活率（%） = (A490 nm樣本/ A490 nmDMSO處理的細(xì)胞 × 100)。
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 BIIB021口服處理多種移植瘤模型（包括N87, BT474, CWR22, U87, SKOV3和 Panc-1）導(dǎo)致腫瘤生長(zhǎng)受抑制。[1] BIIB021按120 mg/kg劑量處理 L540cy 腫瘤，有效抑制腫瘤的生長(zhǎng)。[2] BIIB021 作用于JHU12移植瘤，明顯增強(qiáng)抗腫瘤生長(zhǎng)功效。[3]
動(dòng)物實(shí)驗(yàn) Animal Models BALB/c和無胸腺鼠中的N87, BT474, CWR22, U87, SKOV3和 Panc-1腫瘤模型
Dosages 31, 62.5,和125 mg/kg
Administration 每天口服處理一次
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01017198 Completed
Advanced Solid Tumors
Biogen
 November 2009 Phase 1
NCT01004081 Completed
Breast Cancer
Biogen
 November 2009 Phase 2
NCT00618735 Completed
Advanced Solid Tumors
Biogen
 February 2008 Phase 1
NCT00618319 Completed
GIST
Biogen
 February 2008 Phase 2

化學(xué)信息&溶解度

分子量 318.76 分子式

C14H15ClN6O
CAS號(hào) 848695-25-0 SDF Download BIIB021 SDF
Smiles CC1=CN=C(C(=C1OC)C)CN2C=NC3=C2N=C(N=C3Cl)N
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 64 mg/mL ( (200.77 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 12 mg/mL (37.64 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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