Carfilzomib (PR-171)

中文名称:卡非佐米

Carfilzomib (PR-171) 是一种不可逆proteasome抑制剂,在ANBL-6细胞中IC50为<5 nM,在体外优先抑制β5亚基的ChT-L活性,对PGPH和T-L活性很弱或没有作用。Carfilzomib 可激活自噬并诱导细胞凋亡。

Carfilzomib (PR-171) Chemical Structure

Carfilzomib (PR-171) Chemical Structure

CAS: 868540-17-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
5mg RMB 647.01 现货
50mg RMB 3104.01 现货
100mg RMB 4823.91 现货
200mg RMB 7690.41 现货
1g RMB 13677.3 现货
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客户使用Selleck的Carfilzomib (PR-171)发表文献205

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批次: 纯度: 99.75%
99.75

Carfilzomib (PR-171)相关产品

相关信号通路图

Proteasome抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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

产品描述 Carfilzomib (PR-171) 是一种不可逆proteasome抑制剂,在ANBL-6细胞中IC50为<5 nM,在体外优先抑制β5亚基的ChT-L活性,对PGPH和T-L活性很弱或没有作用。Carfilzomib 可激活自噬并诱导细胞凋亡。
靶点
Proteasome [1]
(ANBL-6 cells)
5 nM
体外研究(In Vitro)
体外研究活性

Carfilzomib抑制多种细胞系和源自患者的肿瘤细胞的增殖,包括多发性骨髓瘤。Carfilzomib诱导内在和外在的凋亡信号传导途径并激活c-Jun N-末端激酶(JNK)。与bortezomib相比,Carfilzomib协同地塞米松(Dex)表现增强的抗MM活性,并克服了bortezomib等药物的抗性。 Carfilzomib有选择地抑制β5亚基的CHT- L活性,在10 nM剂量时抑制超过80%的活性。低剂量Carfilzomib短期处理导致优先结合特异性的β5组成20S蛋白酶体和β5i免疫蛋白酶体亚基。在Carfilzomib刺激的ANBL -6细胞中检测caspase活性,结果显示caspase- 8和caspase -9和caspase-3活性在8小时后大幅增加,和对照8小时后的细胞相比分别增加了3.2 , 3.9和6.9倍。在carfilzomib处理过的细胞中,线粒体膜的完整性减少到41%(Q1 + Q2),而在对照细胞中这一比例为75%。[1] 在另一项研究中,Carfilzomib也表现出对血液和实体肿瘤的临床前有效性。[2] Carfilzomib直接一直破骨形成和骨吸收。[3]

激酶实验 酶联免疫吸附试验分析carfilzomib亚基
ANBL -6细胞(2 ×106/孔)接种于96孔板中并用Carfilzomib(0.001至10μM)处理 1小时。然后将细胞裂解(20mM的Tris-HCl, 0.5 mM EDTA),并裂解物上清转移到聚合酶链反应(PCR)平板上。使用起始浓度为6 μg/μL处理ANBL - 6细胞得到的裂解物做标准曲线。活性位点探针[生物素-(CH2)4-Leu-Leu-Leu-环氧酮; 20 μM]加入并于室温温育1小时。在细胞裂解液中添加1%十二烷基硫酸钠(SDS)和加热至100℃变性 ,随后在96孔的多屏DV板中每孔和20μL链霉亲和琼脂糖高性能珠混合并孵育1小时。这些珠粒用酶联免疫吸附试验(ELISA)缓冲液(PBS,1%牛血清白蛋白和0.1 %吐温-20)洗涤细胞,并温育过夜,在4℃在板振荡器上与抗体的蛋白酶体亚基反应。所用抗体包括鼠单克隆抗- β1 ,抗-β2 ,抗β1i和抗β5i ,山羊多克隆抗β2i ,和兔多克隆抗- β5 (针对KLH- CWIRVSSDNVADLHDKYS肽亲和纯化的抗血清)。珠粒洗涤后用以辣根过氧化物酶标记的二羊抗兔,羊抗鼠或兔antigoat抗体温育2小时。洗涤后,将珠粒用SuperSignal ELISA picochemiluminescence底物反应,而后进行荧光检测。荧光信号通过与标准曲线比较转换为μg/mL,表示为抑制相对于对照的%。使用以下nonsigmoidal剂量 - 反应方程生成拟合曲线:Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope)),其中X是浓度的对数, Y是抑制%,EC 50是表示50%的效果的剂量。
细胞实验 细胞系 WST-1, ANBL-6细胞
浓度 100 nM
孵育时间 1小时
方法

WST-1被用于确定蛋白酶体抑制剂Carfilzomib对细胞增殖的影响。增殖的抑制作用是与对照细胞比较所得。线性样条函数是用来使用XLfit4软件进行计算半数抑制浓度(IC50)。抗性程度(DOR)的计算公式是IC50(抗性细胞)/ IC50(敏感细胞)。 ANBL-6细胞用100nM carfilzomib短暂处理,洗涤并悬浮于含有5μg/mL JC-1PBS中,它显示出在线粒体电位依赖性积聚。用FACScan分析线粒体膜电位依赖性颜色转变(从525到590 nM),数据用CellQuest软件分析。

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性

Carfilzomib适度降低了体内异种移植物模型中肿瘤的生长。在持续或短暂处理下, Carfilzomib有效地降低多发性骨髓瘤细胞活力。 Carfilzomib增加骨小梁体积,减少骨吸收,并提高非肿瘤小鼠的骨形成。[3]

动物实验 Animal Models Beige-nude-XID小鼠
Dosages 2.0 mg/kg
Administration 静脉注射
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 --

化学信息&溶解度

分子量 719.91 分子式

C40H57N5O7

CAS号 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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (138.9 mM); DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 50 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 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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