SNS-032 (BMS-387032)

For research use only. Not for use in humans.

目录号：S1145

SNS-032 (BMS-387032) Chemical Structure

CAS No. 345627-80-7

SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂，无细胞试验中IC50为48 nM，比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感，IC50为62 nM/4 nM，对CDK6几乎没有抑制效果。SNS-032 (BMS-387032)可诱导凋亡。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1414.37 现货
RMB 901.17 现货
RMB 4675.34 现货
RMB 13677.3 现货
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客户使用Selleck生产的SNS-032 (BMS-387032)发表文献66篇：

产品安全说明书

CDK抑制剂选择性比较

生物活性

产品描述 SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂，无细胞试验中IC50为48 nM，比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感，IC50为62 nM/4 nM，对CDK6几乎没有抑制效果。SNS-032 (BMS-387032)可诱导凋亡。Phase 1。
特性 SNS-032是新一代CDK抑制剂,具有更高的选择性和更弱的毒性。
靶点
CDK9/CyclinT [3]
(Cell-free assay)		 CDK2/CyclinA [3]
(Cell-free assay)		 CDK2/CyclinE [1]
(Cell-free assay)		 CDK7/CyclinH [3]
(Cell-free assay)		 GSK-3α [3]
(Cell-free assay)
4 nM 38 nM 48 nM 62 nM 230 nM
体外研究

SNS-032是新型有效的选择性Cdk抑制剂, 有效抑制Cdk2, Cdk7和Cdk9。体外，不管病情预断和治疗病史如何，SNS-032都可有效杀死慢性淋巴细胞性白血病细胞。与Flavopiridol和Roscovitine相比, 抑制RNA合成和诱导细胞凋亡时，SNS-032更有效。SNS-032是可逆的，使SNS-032重激活RNA聚合酶II失活, 导致Mcl-1再合成和细胞存活。[1] SNS-032抑制内皮细胞的三维毛细管网形成。SNS-032作用于人脐静脉内皮细胞(HUVECs),完全抑制U87MG细胞调节的毛细管形成。此外, SNS-032明显抑制VEGF的产生,从而抑制血管生成。临床前期研究显示SNS-032跨多种细胞系诱导细胞周期停滞和细胞凋亡。[2]SNS-032通过抑制 CDKs 2和7而阻断细胞周期, 通过抑制CDKs 7和9阻断转录。SNS-032的活性不受人类血清影响。[3] SNS-032诱导膜联蛋白V染色增多和caspase-3激活，这种作用存在剂量依赖性。在分子水平, SNS-032诱导RNA多聚酶(RNA Pol) II 在serine 2和5位点去磷酸化。且抑制CDK2，CDK9。和去磷酸化的CDK7的表达。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2780 cell line M3XFVnBzd2yrZnXyZZRqd25iYYPzZZk> M1LxeVczKGh? NEfjWIxCdnSrcILvcIln\XKjdHn2[UBm\m[nY4SgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuIHzpcoUhf2G|IHTleIVzdWmwZXSgbY4h[SC5aH;s[UBk\WyuIEeyJIhzKGO7dH;0c5hq[2m2eTDhd5NigSxiSVO1NF06PSCwTR?= NWTrNIxiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWwNlc5PjNpPkG1NFI4QDZ|PD;hQi=>
Sf21 M4XMU2Z2dmO2aX;uJIF{e2G7 NV7ieI9HUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBENXSncn3pcoFtKEirc{[teIFo\2WmIFPET|kw[3mlbHnuJHQyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jJzIHnud4VkfCClZXzsd{B2e2mwZzDQSGt1cWSnIHHzJJN2[nO2cnH0[UwhUUN3ME2wMlAxPM7:TR?= MmLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Sf21 NH;QWotHfW6ldHnvckBie3OjeR?= MnXqTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCFLYTldo1qdmGuIFjpd|YufGGpZ3XkJGNFUzJxTj30[ZJucW6jbDDHV3QufGGpZ3XkJIN6[2yrbjDBJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lIyKGmwc3XjeEBk\WyuczD1d4lv\yCqaYP0c45mKEhzIHHzJJN2[nO2cnH0[UwhUUN3ME2wMlA{QM7:TR?= M2jUfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUexNFM3Lz5{N{G3NVA{PjxxYU6=
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HCT116 Mk\LSpVv[3Srb36gZZN{[Xl? Ml3ONVYhcHK| M1vQW2lvcGmkaYTpc44hd2ZiQ1TLPU1u\WSrYYTl[EBTVkFicH;sJFIheGixc4Doc5J6dGG2aX;uJIF1KHOnckKgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFE3KGi{czDifUBJS1NiYYPzZZktKEmFNUC9NE42Pc7:TR?= MlXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7Mk[2PVkoRjF6OUK2Olk6RC:jPh?=
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Sf cells NXj0VJFJTnWwY4Tpc44h[XO|YYm= NGLqRYhKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBETEt2L3P5Z4xqdiCGMTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRic3[gZ4VtdHNuIFnDOVA:OC57MkZOwG0> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
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NB1643 NFzHSmhyUFSVIHHzd4F6 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM> M1jGNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NIf2OoJyUFSVIHHzd4F6 MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=> NUD5U5h7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC M{P4[pFJXFNiYYPzZZk> NU[yeGZoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= Ml7yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 MWjxTHRUKGG|c3H5 NUnTNlZWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NXPXc5J7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 M4LUW5FJXFNiYYPzZZk> M{i2b5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGxCVi13IHPlcIx{ MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY MWXxTHRUKGG|c3H5 NF\hOFlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBFSU:\IHPlcIx{ MnzLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MlfvdWhVWyCjc4PhfS=> NIXpS|FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| NID2UJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 MVjxTHRUKGG|c3H5 M3PRN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ NVLzSoRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 NH34e4RyUFSVIHHzd4F6 MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS NV;qXFVmeUiWUzDhd5NigQ>? MmnBdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ NFzReno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NEHu[4JyUFSVIHHzd4F6 M3fqUpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NYO0XnV{eUiWUzDhd5NigQ>? M1fEeZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJFKGOnbHzz MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 M3Pr[JFJXFNiYYPzZZk> Ml60dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ M1Ln[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NH;LfmdyUFSVIHHzd4F6 Mnj1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgU2hUNTVyIHPlcIx{ NVLOOIVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NF[wdW1yUFSVIHHzd4F6 M{Dzd5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? M4KxfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-RNA PolII / RNA Pol II / CDK7 / CDK9 ; 

PubMed: 31526394     


SNS-032 inhibited CTD phosphorylation of RNA Pol II in UM cells. Cells were treated with increasing concentration of SNS-032 for 48 h, Western blot analysis with the indicated antibodies was performed.

YAP / p-YAP / CTGF / CYR61 ; 

PubMed: 31526394     


SNS-032 blocked YAP signaling in UM cells. Mel270 and Omm2.3 cells were treated with SNS-032 for 48 h, the protein levels of YAP, phospho-YAP (S127) and its downstream targets CTGF and CYR61 were examined by Western blot analysis. 

p-ROCK / ROCK / p-LIMK1/2 / LIMK1/2 / p-Cofilin / Cofilin ; 

PubMed: 31526394     


SNS-032 inhibited the RhoA-ROCK-LIMK1/2-cofilin pathway. Mel270 and Omm2.3 cells were treated with increasing concentrations of SNS-032 for 48 h, and then subjected to Western blot analysis with the indicated antibodies.

Mcl-1 / Cyclin D1 / Bcl-2 / PARP ; 

PubMed: 20663900     


SNS-032 reduced the protein levels of Mcl-1 and cyclin D1 and induced apoptosis.

31526394 20663900
Growth inhibition assay
Cell viability; 

PubMed: 20663900     


SNS-032 inhibited proliferation of the four MCL cell lines. MCL cells were seeded on 24 well plates, SNS-032 at concentrations of 0 (○), 0.03, (●), 0.1 (◆), 0.3 (▼), 1 (▲) and 3 (■) μM were added the next day. Cell concentrations were measured at 24, 48 and 72 h after addition of SNS-032. Data (mean +/− SD) represent percentage of cell growth compared to day 1 of three independent experiments.

20663900
体内研究 SNS-032作用于肿瘤共培养模型，阻断肿瘤细胞诱导的VEGF分泌。[2] SNS-032, 作用于实体瘤时具有更高选择性，且毒性较弱。[4]

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：[2]
- 合并
  • Cell lines: HUVECs和U87MG细胞
  • Concentrations: 0-0.5 mM
  • Incubation Time: 24, 48, 或72小时
  • Method: U87MG细胞和HUVECs (每孔2000个细胞)接种在96孔板上，终体积为100 ml。24小时后,用不同浓度SNS-032(0-0.5 mM)处理细胞24,48,或72小时。完全处理后, 每孔加入100 mL CTG溶液，室温下黑暗温育20分钟。50 mL溶解物转移到96孔板上，通过POLARstar OPTIMA测定荧光值。计算加入SNS-032后的细胞生长百分数。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 76 mg/mL (199.72 mM)
Water Insoluble
Ethanol 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)：
30% PEG400+0.5% Tween80+5% propylene glycol
 30 mg/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 380.53
化学式

C17H24N4O2S2
CAS号 345627-80-7
储存条件 粉状
溶于溶剂
别名 N/A

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）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
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
计算重置

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、SDS / 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、SDS / 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
NCT00446342 Completed Drug: SNS-032 Injection B-lymphoid Malignancies|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Multiple Myeloma Sunesis Pharmaceuticals February 2007 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

  • 活性最高的CDK抑制剂

    LY2835219 : CDK4, IC50=2 nM; CDK6, IC50=10 nM.

  • 用于临床的CDK抑制剂

    Palbociclib (PD0332991) Isethionate : Phase III for Metastatic Breast Cancer.

  • 最新的CDK抑制剂

    NU6027 : Potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

相关CDK产品

  • SU9516 New

    SU9516是一种3位取代的吲哚酮类CDK抑制剂，对CDK2，CDK1，和CDK4的IC50分别为22 nM，40 nM，和200 nM。

  • Ro-3306 New

    RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂，Ki 为20 nM，选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。

  • Purvalanol A New

    Purvalanol A 是一种有效的，细胞渗透性 CDK 抑制剂，对cdc2-cyclin B，cdk2-cyclin A，cdk2-cyclin E，和 cdk4-cyclin D1的 IC50 分别为 4 nM，70 nM，35 nM，和 850 nM。Purvalanol A 可诱导内质网应激介导的凋亡与自噬。

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。Phase 3。

    Features:PD-0332991作为有应用前景的工具测定CDK激酶是否具有明显的治疗价值。

  • Palbociclib (PD0332991) Isethionate

    Palbociclib (PD0332991) Isethionate是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50为11 nM/16 nM，对CDK1/2/5，EGFR，FGFR，PDGFR， InsR等没有抑制活性。Phase 3。

    Features:PD 0332991治疗多种癌症，特异性抑制CDK4/6，是第一种有前途的抑制剂。

  • Dinaciclib (SCH727965)

    Dinaciclib (SCH727965, PS-095760) 是一种新型有效的CDK抑制剂，作用于CDK2，CDK5，CDK1和CDK9，无细胞试验中IC50分别为1 nM，1 nM，3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Dinaciclib 可通过激活caspases 8和caspases 9来诱导细胞凋亡。Phase 3。

    Features:[1]

  • Flavopiridol (L86-8275) HCl

    Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033)与ATP竞争性抑制CDKs，作用于CDK1，CDK2，CDK4和CDK6，无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。

  • Roscovitine (CYC202)

    Roscovitine (CYC202, Seliciclib, R-roscovitine)是一种有效的，选择性CDK抑制剂，作用于Cdc2，CDK2和CDK5时，无细胞试验中IC50分别为0.65 μM，0.7 μM和0.16 μM，对CDK4/6几乎没有作用。Phase 2。

  • Abemaciclib mesylate (LY2835219)

    Abemaciclib (LY2835219)是一种有效的，选择性CDK4和CDK6抑制剂，无细胞试验中IC50分别为2 nM和10 nM。Phase 3。

  • Ribociclib (LEE011)

    Ribociclib (LEE011) 是一种具有口服活性的、高度特异性的CDK4和CDK6抑制剂，对应的IC50值分别为10 nM和39 nM。Phase 3。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID