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Carfilzomib (PR-171)

中文名稱：卡非佐米

Carfilzomib (PR-171) 是一種不可逆proteasome抑制劑，在ANBL-6細(xì)胞中IC50為<5 nM，在體外優(yōu)先抑制β5亞基的ChT-L活性，對PGPH和T-L活性很弱或沒有作用。Carfilzomib 可激活自噬并誘導(dǎo)細(xì)胞凋亡。

Carfilzomib (PR-171) Chemical Structure

Carfilzomib (PR-171) Chemical Structure

CAS: 868540-17-4

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
5mg 647.01 現(xiàn)貨
50mg 3104.01 現(xiàn)貨
200mg 7690.41 現(xiàn)貨
1g 13677.3 現(xiàn)貨
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Carfilzomib (PR-171)相關(guān)產(chǎn)品

相關(guān)信號通路圖

Proteasome Signaling Pathways

Proteasome信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
UMSCC-1 Apoptosis Asssay 200 nM 24 h induce the cell apoptosis co-treatment with ONX 0912 22929803
1483 Apoptosis Asssay 200 nM 24 h induce the cell apoptosis co-treatment with ONX 0912 22929803
UMSCC-22B Apoptosis Asssay 200 nM 24 h induce the cell apoptosis co-treatment with ONX 0912 22929803
UMSCC-22A Apoptosis Asssay 200 nM 24 h induce the cell apoptosis co-treatment with ONX 0912 22929803
Jurkat Apoptosis Asssay 8 nM 24/48 h induces apoptosis, caspase activation, and PARP cleavage co-treatment with vorinostat 24801128
Jurkat Growth Inhibition Assay 1-11nM 48 h inhibits the cell proliferation co-treatment with vorinostat 24801128
U2932 Apoptosis Asssay 2.5–3.5 nM 48 h enhances the cell death co-treatment with ACY1215 25239935
SUDHL14 Apoptosis Asssay 2.5–3.5 nM 48 h enhances the cell death co-treatment with ACY1215 25239935
SUDHL16? Apoptosis Asssay 2.5–3.5 nM 48 h enhances the cell death co-treatment with ACY1215 25239935
NCI-H929? Growth Inhibition Assay 0-100 nM 48 h IC50 =?14 nM 25312543
MM.1S Growth Inhibition Assay 0-100 nM 48 h IC50?=?10 nM 25312543
SUDHL16 Apoptosis Asssay 2.0-4.0 nM 48 h induces cell death co-treatment with obatoclax 22411899
SUDHL16 Function Assay 2.5 nM 24 h activates JNK, inactivates AKT, up-regulates Noxa, and induces γH2A.X co-treatment with obatoclax 22411899
Granta Growth Inhibition Assay 0-4 nM 48 h induce cell death co-treatment with HADCIs 21750224
SUDHL16 Growth Inhibition Assay 1-4 nM 36 h induce cell death co-treatment with HADCIs 20233973
MCF7 Function assay 35 nM 4 hrs Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis 27994734
MDA-MB-468 Function assay 35 nM 4 hrs Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis 27994734
MOLT4 Function assay 1 hr Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay, IC50 = 0.0051 μM. 19348473
MESSA Cytotoxicity assay 72 hrs Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.018 μM. 19348473
MESSA Cytotoxicity assay 72 hrs Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.413 μM. 19348473
RPMI8226 Cytotoxicity assay 72 hrs Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay, IC50 = 0.01319 μM. 24767818
NCI-H929 Cytotoxicity assay 72 hrs Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay, IC50 = 0.02132 μM. 24767818
CCRF-CEM Antiproliferative assay 72 hrs Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0061 μM. 26231162
RPMI8266 Antiproliferative assay 72 hrs Antiproliferative activity against human RPMI8266 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0139 μM. 26231162
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0193 μM. 26231162
A431 Antiproliferative assay 72 hrs Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM. 26231162
TOV21G Antiproliferative assay 72 hrs Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM. 26231162
RKO Antiproliferative assay 72 hrs Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0271 μM. 26231162
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM. 27765408
RPMI8226 Antiproliferative assay 72 hrs Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM. 27765408
LCL Cytotoxicity assay 48 hrs Cytotoxicity against human LCL cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.03 μM. 27994734
RD-ES Cytotoxicity assay 48 hrs Cytotoxicity against human RD-ES cells harboring p53 mutant assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.043 μM. 27994734
U266 Cytotoxicity assay 48 hrs Cytotoxicity against human U266 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.06 μM. 27994734
WE68 Cytotoxicity assay 48 hrs Cytotoxicity against human WE68 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.08 μM. 27994734
IMR90 Cytotoxicity assay 48 hrs Cytotoxicity against human IMR90 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.13 μM. 27994734
MCF10A Cytotoxicity assay 48 hrs Cytotoxicity against human MCF10A cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM. 27994734
SKOV3 Cytotoxicity assay 48 hrs Cytotoxicity against p53 deficient human SKOV3 cells assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM. 27994734
MDA-MB-468 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-468 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.33 μM. 27994734
HNDF Cytotoxicity assay 48 hrs Cytotoxicity against HNDF cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.35 μM. 27994734
KGN Cytotoxicity assay 48 hrs Cytotoxicity against human KGN cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.45 μM. 27994734
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 4.5 μM. 27994734
MM1S Cytotoxicity assay 72 hrs Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM. 28027531
RPMI8226 Cytotoxicity assay 72 hrs Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM. 28027531
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.0041 μM. 30165344
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.0044 μM. 30165344
RPMI8226 Cytotoxicity assay 48 hrs Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay, IC50 = 0.0067 μM. 30165344
UMSCC-22A Growth Inhibition Assay IC50=38.7 ± 1.0 nM 22929803
R-Cal33 Growth Inhibition Assay IC50=1112 nM 24915039
P-Cal33 Growth Inhibition Assay IC50=17.3 nM 24915039
R-UMSCC-1 Growth Inhibition Assay IC50=2294 nM 24915039
P-UMSCC-1 Growth Inhibition Assay IC50=11.2 nM 24915039
UMSCC-22B Growth Inhibition Assay IC50=30.7 ± 9.3 nM 22929803
1483 Growth Inhibition Assay IC50=50.5 ± 11.9 nM 22929803
UMSCC-1 Growth Inhibition Assay IC50=34.6 ± 2.6 nM 22929803
Cal33 Growth Inhibition Assay IC50=49.3 ± 8.9 nM 22929803
PCI-15A Growth Inhibition Assay IC50=70.4 ± 22.6 nM 22929803
PCI-15B Growth Inhibition Assay IC50=39.5 ± 11.0 nM 22929803
OSC-19 Growth Inhibition Assay IC50=18.3 ± 4.2 nM 22929803
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells 29435139
Daoy qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) 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
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
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
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells 29435139
ANBL-6 Function assay Inhibition of 20S proteasome activity in human ANBL-6 cells, IC50 = 0.01 μM. 29652143
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生物活性

產(chǎn)品描述 Carfilzomib (PR-171) 是一種不可逆proteasome抑制劑，在ANBL-6細(xì)胞中IC50為<5 nM，在體外優(yōu)先抑制β5亞基的ChT-L活性，對PGPH和T-L活性很弱或沒有作用。Carfilzomib 可激活自噬并誘導(dǎo)細(xì)胞凋亡。
靶點(diǎn)
Proteasome [1]
(ANBL-6 cells)
5 nM
體外研究(In Vitro)
體外研究活性

Carfilzomib抑制多種細(xì)胞系和源自患者的腫瘤細(xì)胞的增殖，包括多發(fā)性骨髓瘤。Carfilzomib誘導(dǎo)內(nèi)在和外在的凋亡信號傳導(dǎo)途徑并激活c-Jun N-末端激酶(JNK)。Carfilzomib協(xié)同地塞米松(Dex)表現(xiàn)增強(qiáng)的抗MM活性，并克服了藥物的抗性。 Carfilzomib有選擇地抑制β5亞基的CHT- L活性，在10 nM劑量時抑制超過80％的活性。低劑量Carfilzomib短期處理導(dǎo)致優(yōu)先結(jié)合特異性的β5組成20S蛋白酶體和β5i免疫蛋白酶體亞基。在Carfilzomib刺激的ANBL -6細(xì)胞中檢測caspase活性，結(jié)果顯示caspase- 8和caspase -9和caspase-3活性在8小時后大幅增加，和對照8小時后的細(xì)胞相比分別增加了3.2 ， 3.9和6.9倍。在carfilzomib處理過的細(xì)胞中，線粒體膜的完整性減少到41%(Q1 + Q2)，而在對照細(xì)胞中這一比例為75％。[1] 在另一項研究中，Carfilzomib也表現(xiàn)出對血液和實體腫瘤的臨床前有效性。[2] Carfilzomib直接一直破骨形成和骨吸收。[3]
激酶實驗 酶聯(lián)免疫吸附試驗分析carfilzomib亞基
ANBL -6細(xì)胞（2 ×106/孔）接種于96孔板中并用Carfilzomib（0.001至10μM）處理 1小時。然后將細(xì)胞裂解（20mM的Tris-HCl， 0.5 mM EDTA），并裂解物上清轉(zhuǎn)移到聚合酶鏈反應(yīng)（PCR）平板上。使用起始濃度為6 μg/μL處理ANBL - 6細(xì)胞得到的裂解物做標(biāo)準(zhǔn)曲線。活性位點(diǎn)探針[生物素-(CH2)4-Leu-Leu-Leu-環(huán)氧酮; 20 μM]加入并于室溫溫育1小時。在細(xì)胞裂解液中添加1％十二烷基硫酸鈉（SDS）和加熱至100℃變性 ，隨后在96孔的多屏DV板中每孔和20μL鏈霉親和瓊脂糖高性能珠混合并孵育1小時。這些珠粒用酶聯(lián)免疫吸附試驗(ELISA)緩沖液（PBS，1％牛血清白蛋白和0.1 ％吐溫-20）洗滌細(xì)胞，并溫育過夜，在4℃在板振蕩器上與抗體的蛋白酶體亞基反應(yīng)。所用抗體包括鼠單克隆抗- β1 ，抗-β2 ，抗β1i和抗β5i ，山羊多克隆抗β2i ，和兔多克隆抗- β5 （針對KLH- CWIRVSSDNVADLHDKYS肽親和純化的抗血清）。珠粒洗滌后用以辣根過氧化物酶標(biāo)記的二羊抗兔，羊抗鼠或兔antigoat抗體溫育2小時。洗滌后，將珠粒用SuperSignal ELISA picochemiluminescence底物反應(yīng)，而后進(jìn)行熒光檢測。熒光信號通過與標(biāo)準(zhǔn)曲線比較轉(zhuǎn)換為μg/mL，表示為抑制相對于對照的％。使用以下nonsigmoidal劑量 - 反應(yīng)方程生成擬合曲線：Y = Bottom + (Top-Bottom)/(1 + 10?((LogEC50 ? X) × HillSlope))，其中X是濃度的對數(shù)， Y是抑制％，EC 50是表示50％的效果的劑量。
細(xì)胞實驗 細(xì)胞系 WST-1, ANBL-6細(xì)胞
濃度 100 nM
孵育時間 1小時
方法

WST-1被用于確定蛋白酶體抑制劑Carfilzomib對細(xì)胞增殖的影響。增殖的抑制作用是與對照細(xì)胞比較所得。線性樣條函數(shù)是用來使用XLfit4軟件進(jìn)行計算半數(shù)抑制濃度（IC50）?？剐猿潭?DOR)的計算公式是IC50（抗性細(xì)胞）/ IC50（敏感細(xì)胞）。 ANBL-6細(xì)胞用100nM carfilzomib短暫處理，洗滌并懸浮于含有5μg/mL JC-1PBS中，它顯示出在線粒體電位依賴性積聚。用FACScan分析線粒體膜電位依賴性顏色轉(zhuǎn)變（從525到590 nM），數(shù)據(jù)用CellQuest軟件分析。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot pERK / ERK / pSTAT5 / STAT5 / pPI3K / PI3K caspase-9 / caspase-8 c-PARP / PARP / caspase-3 Bcl-2 / Bcl-Xl / Mcl-1 / Bik / Bim / Bax / Bak Atg5 / Atg12 / Beclin-1 / LC3-II Noxa / Bik / Puma / Mcl-1 EGFR / HER2 / ER alpha / p-Akt(Ser473) / Akt / p-ERK / ERK / p53 BDP1 / HER2(Tyr1248) / HER2(Tyr1221/Tyr1222) / PARP1 / caspase-7 / p53 Mut HLA class I 24590311
Growth inhibition assay Cell viability 27655642
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Carfilzomib適度降低了體內(nèi)異種移植物模型中腫瘤的生長。在持續(xù)或短暫處理下， Carfilzomib有效地降低多發(fā)性骨髓瘤細(xì)胞活力。 Carfilzomib增加骨小梁體積，減少骨吸收，并提高非腫瘤小鼠的骨形成。[3]
動物實驗 Animal Models Beige-nude-XID小鼠
Dosages 2.0 mg/kg
Administration 靜脈注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05552976 Recruiting
Relapsed or Refractory Multiple Myeloma
Bristol-Myers Squibb
 January 10 2023 Phase 3
NCT05675449 Recruiting
Multiple Myeloma
Pfizer
 December 14 2022 Phase 1
NCT05041933 Unknown status
Hematological Diseases
University Hospital Limoges
 September 15 2021 --

化學(xué)信息&溶解度

分子量 719.91 分子式

C40H57N5O7
CAS號 868540-17-4 SDF Download Carfilzomib (PR-171) SDF
Smiles CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (138.9 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 50 mg/mL (69.45 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

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

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(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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常見問題及建議解決方法

問題 1:
How should I prepare solution of Carfilzomib for ongoing in vivo study?

回答：
This compound can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/ml as a suspension, and can be dissolved in 2% DMSO/ castor oil at 10 mg/ml as a clear solution.

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