selinexor(KPT-330)

For research use only. Not for use in humans.

目录号:S7252 别名: ATG-010

selinexor(KPT-330) Chemical Structure

Molecular Weight(MW): 443.31

Selinexor (KPT-330)是一种口服生物有效的选择性CRM1抑制剂。Phase 2。

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客户使用Selleck生产的selinexor(KPT-330)发表文献19篇:

产品安全说明书

CRM1抑制剂选择性比较

生物活性

产品描述 Selinexor (KPT-330)是一种口服生物有效的选择性CRM1抑制剂。Phase 2。
靶点
CRM1 [1]
(Cell-free assay)
体外研究

KPT-330作为KPT-185的临床候选药,对T-ALL细胞的存活具有相似的作用效果,并迅速引发凋亡反应。KPT-330也降低MOLT-4,Jurkat,HBP-ALL,KOPTK-1,SKW-3,和DND-41细胞系生长,IC50为34-203 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT474 cells M3rCOmZ2dmO2aX;uJIF{e2G7 NUnx[|dIOC5zIN88US=> NGT5UFgzPCCqIH;yJFQ5KGh? NIjoUIJqdmS3Y3XzJIRq\m[ncnXueIlidCCDa4Sgd4lodmGuaX7nMUBidmRibXX0ZYJwdGm|bT3hd5Nw[2mjdHXkJIdmdmViZYjwdoV{e2mxbjDwdo9ncWyncz6= M2DT[FMxQTh5M{iw
MCF-7 NXjTbIRUTnWwY4Tpc44h[XO|YYm= MnHsNE4yKM7:TR?= NWfaOGdUOjRiaDDvdkA1QCCq MVTpcoR2[2W|IHTp[oZmemWwdHnhcEBCc3Ric3nncoFtcW6pLTDhcoQhdWW2YXLvcIl{dS2jc4PvZ4lifGWmIHflcoUh\XiycnXzd4lwdiCycn;mbYxmey5? NV73codEOzB7OEezPFA>
THP-1 M1yydGZ2dmO2aX;uJIF{e2G7 MUiyOEBp NInnT|REdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmKDNid3Xy[UB{fHKxbnfsfUBmdmijbnPl[EBqdiC2aHWgZ49u[mmwYYTpc44hfHKnYYTt[Y51KHeqZX6gZ49ueGG{ZXSgeI8hSUKWLUG5PUBweiCNUGStN|MxKGGub37l NWD6bohYOzB3OU[zPVg>
OCI-AML3 MUDGeY5kfGmxbjDhd5NigQ>? Ml;PNlQhcA>? MlS2R4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[UA{KHencnWgd5Rzd26pbImg[Y5p[W6lZXSgbY4hfGinIHPvcYJqdmG2aX;uJJRz\WG2bXXueEB4cGWwIHPvcZBiemWmIITvJGFDXC1zOUmgc5IhU1CWLUOzNEBidG:wZR?= Mni3N|A2QTZ|OUi=
MV4-11 NVf3e|FxTnWwY4Tpc44h[XO|YYm= NHHZ[G8zPCCq MoK2R4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[UA{KHencnWgd5Rzd26pbImg[Y5p[W6lZXSgbY4hfGinIHPvcYJqdmG2aX;uJJRz\WG2bXXueEB4cGWwIHPvcZBiemWmIITvJGFDXC1zOUmgc5IhU1CWLUOzNEBidG:wZR?= MUWzNFU6PjN7OB?=
T24 M3rPUWNmdGxidnnhZoltcXS7IHHzd4F6 NWq0W4VpOCxiMD6wNUwhOC5zLDCxJO69VQ>? MljNO|IhcA>? NIPjeldk\WyuII\pZYJqdGm2eTDk[YNz\WG|ZXSgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= Mnf0N|A{PDl4NUC=
J82 MVTD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NVy5e5R1OCxiMD6wNUwhOC5zLDCxJO69VQ>? M1y0PFczKGh? MYDj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{jZWVMxOzR7NkWw
TCCSUP MWHD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MYOwMEAxNjBzLDCwMlEtKDFizszN MlLhO|IhcA>? NHXt[HFk\WyuII\pZYJqdGm2eTDk[YNz\WG|ZXSgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MmH0N|A{PDl4NUC=
UM-UC-3 M3\YUGNmdGxidnnhZoltcXS7IHHzd4F6 NW\qSXJ{OCxiMD6wNUwhOC5zLDCxJO69VQ>? Mn\hO|IhcA>? MmS3Z4VtdCC4aXHibYxqfHliZHXjdoVie2WmIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NWi3Wo15OzB|NEm2OVA>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CHEK1 / MLH1 / MSH2 / PMS2 / Rad51; 

PubMed: 30112106     


Western blot of proteins from whole cell lysates of HT1080 cells treated with 0, 0.1, or 1 μM selinexor and ASPS-KY cells treated with 0, 1, or 10 μM selinexor confirmed the RPPA results suggesting down-regulation of CHEK1, MLH1, MSH2, PMS2 and Rad51 protein levels from selinexor treatment in both cell lines.

XPO1 / Cyclin B1 / Cyclin D1 / c-Myc / c-Met / Mcl-1 / p21 Waf1/Cip1 / p53/ Cleaved PARP / Cleaved caspase-9 / Cleaved caspase-3 / Aurora-B; 

PubMed: 28852098     


OGK-M, HTH83, CAL62 and T238 cells were treated with either selinexor (1,000 nM) or DMSO for 24 h. Lysates were analyzed by western blot analysis for the indicated cell cycle and apoptosis proteins (GAPDH, internal loading control).

AXL / phospho-AKT / phospho-P70S6K / AKT / P70S6K; 

PubMed: 28852098     


HTH83 and CAL62 cells were cultured with either selinexor (1,000 nM) or diluent control (DMSO) for 24 h, and the whole-cell lysate was subjected to western blot analysis for AXL, p-AKT, total AKT, p-P70S6K and total P70S6K.

p53 / CDKN1a / Survivin; 

PubMed: 25948791     


Representative western immunoblotting showing nuclear and cytosolic fractions of XPO1/ CRM1, p53, CDKN1a and survivin in DMPM cells exposed to selinexor (IC50). β-actin and TBP were used to confirm equal protein loading on the gel and to show the relative purity of the nuclear fractions.

30112106 28852098 25948791
Immunofluorescence
XPO1 / tubulin; 

PubMed: 30349650     


Immunofluorescent detection of XPO1 (green) in cells treated with vehicle and selinexor. Cells were plated on chamber slides and they were treated with either vehicle or selinexor for 48 hours. Tubulin (red) and DAPI (blue) served to define the nuclear and cytoplasmic compartment, respectively. V = vehicle, S = selinexor.

NPM1 / PU.1; 

PubMed: 30015632     


IF for NPM1 and PU.1 in vehicle- versus selinexor-treated NPM1-mutated AML cells. DAPI was used to stain for nuclei. Images by Nikon Eclipse 400 microscope; original magnification, ×630.

30349650 30015632
Growth inhibition assay
Cell viability; 

PubMed: 28852098     


Cells were treated with selinexor at indicated concentrations for 72 h, and growth inhibition was measured by MTT assay. Results are expressed as mean value ± SD; n = 4. 

28852098
体内研究 在体内,KPT-330显著抑制T-ALL细胞(MOLT-4)和AML细胞(MV4-11)生长,对正常造血细胞几乎没有毒性。[1] KPT-330处理含弥漫性人类多发性骨髓瘤(MM)骨损害的SCID小鼠,抑制MM诱导的骨溶解,并延长寿命。此外,KPT-330通过抑制RANKL诱导的NF-κB和NFATc1,直接损害破骨细胞形成和骨吸收,对成骨细胞和BMSCs影响极低。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3,和 DND-41细胞系
  • Concentrations: ~1 μM
  • Incubation Time: 72小时
  • Method: 细胞系培养在RPMI1640培养基中,补充10%胎牛血清和青霉素/链霉素。 Cell Titer Glo 测定法用于评估DMSO或KPT-330处理的细胞生存力。细胞按每孔10000个接种在96孔板中,与DMSO或浓度不断增加的KPT-330温育。72 小时后,测量KPT-330处理的细胞存活率,记为对照组DMSO处理细胞的百分比。使用MSCV-IRES-GFP逆转录病毒表达系统获得过表达BCL2的Jurkat细胞。感染BCL2或对照载体病毒的Jurkat细胞通过流式细胞仪进行排序,使用BCL2抗体,通过Western blot分析验证BCL2的表达。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: T-ALL 和 AML 移植瘤小鼠模型
  • Formulation: Pluronic F-68/PVP-K29/32
  • Dosages: 20 -25 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 88 mg/mL (198.5 mM)
Ethanol 40 mg/mL (90.23 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+40%PEG 300+5% Tween80 +ddH2O
4mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 443.31
化学式

C17H11F6N7O

CAS号 1393477-72-9
储存条件 粉状
溶于溶剂
别名 ATG-010

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02091245 Active not recruiting Drug: KPT-330 Relapsed Acute Lymphoblastic Leukemia (ALL)|Refractory Acute Lymphoblastic Leukemia (ALL)|Relapsed Acute Myelogenous Leukemia (AML)|Refractory Acute Myelogenous Leukemia (AML)|Relapsed Mixed Lineage Leukemia|Refractory Mixed Lineage Leukemia|Relapsed Biphenotypic Leukemia|Refractory Biphenotypic Leukemia|Chronic Myelogenous Leukemia (CML) in Blast Crisis Dana-Farber Cancer Institute|William Lawrence and Blanche Hughes Foundation|Karyopharm Therapeutics Inc March 2014 Phase 1
NCT02078349 Unknown status Drug: KPT-330 Solid Tumors National University Hospital Singapore|Karyopharm Therapeutics Inc February 2014 Phase 1
NCT02025985 Completed Drug: Selinexor Ovarian Carcinoma|Endometrial Carcinoma|Cervical Carcinoma|Breast Cancer Karyopharm Therapeutics Inc January 2014 Phase 2
NCT01896505 Completed Drug: KCP-330 Sarcoma Karyopharm Therapeutics Inc July 2013 Phase 1
NCT01607905 Completed Drug: KPT-330 Solid Tumor Karyopharm Therapeutics Inc June 2012 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID