Palbociclib (PD-0332991) HCl

For research use only. Not for use in humans.

Pfizer辉瑞授权 目录号:S1116 中文名称:帕博西尼

Palbociclib (PD-0332991) HCl Chemical Structure

CAS No. 827022-32-2

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。

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RMB 902.49 现货
RMB 1406.17 现货
RMB 4670.26 现货
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客户使用Selleck生产的Palbociclib (PD-0332991) HCl发表文献293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 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。
特性 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。
靶点
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
体外研究

PD 0332991 对其他蛋白激酶包括EGFR, FGFR, PGFR, IR等没有抑制效果。 PD 0332991作用于Cdk4时是非ATP竞争性抑制剂。PD 0332991抑制MDA-MB-435乳腺癌细胞,IC50为66 nM,是由于Rb 在Ser780的磷酸化作用下降。PD 0332991抑制胸苷合并到Rb阳性的人类乳腺癌,结肠癌 肺癌,及白血病的DNA中,IC50值为4 nM到0.17 μM。PD 0332991作用于Rb阴性细胞没有抑制效果。PD 0332991作用于MDA-MB-453乳腺癌细胞和结肠-205细胞使细胞积累在G1期。[1]PD 0332991也有效作用于骨髓瘤5T33MM细胞,使细胞对Bortezomib敏感。[2]PD 0332991抑制luminalER-阳性和HER2-增强的乳腺癌细胞系,包括MDA-MB-175 ZR-75-30 CAMA-1 MDA-MB-134 HCC-202 UACC-893 等等。在这些细胞系中,PD 0332991增强Tamoxifen和Trastuzumab 的活性。在MCF7抗Tamoxifen细胞中,PD 0332991也增强tamoxifen 的敏感性。[3] 最新研究显示PD 0332991可以抑制恶性横纹肌样肿瘤(MRT)细胞系包括MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS,且MRT细胞系对PD 0332991敏感性和p16表达呈负相关。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM13 MV;LbY5ie2ViQYPzZZk> M{jTTFI1KGh? NYnxUJFYUW6qaXLpeIlwdiCxZjDDSGs1KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWmJicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxOiEQvF2= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
COLO205 NGX5NHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzHZ|Y4OiCq NUOzd|JqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkCzOkDPxE1? Mk[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
U937 M2DTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TvWVczKGh? NF34dYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMUSg{txO M3TOfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
MOLM13 NF\yN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUC3NkBp M4DZZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE{KGOnbHzzJIhiemKxcnnu[{BHVFR|IFnUSEBufXSjboSgZZN{\XO|ZXSgZZMhcW6lb4Lwc5JifGmxbjDv[kBcO0ifdHj5cYllcW6nIHnueI8hTE6DIIfpeIghUUN3MDDv[kAxNjB7NjFOwG0> NUP4bGJWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MOLM13 M4qxe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjvPGdzPzJiaB?= M1P5NmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sgd49z[W[nbnniMZJme2m|dHHueEBpfW2jbjDNU2xOOTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkC5OkDPxE1? M1y2TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
MDA-MB-435 MmDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLuR5JiOjRiaB?= MWrJR|UxRTBwMU[g{txO NInWV2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUiwNVg{OSd-MUW4NFE5OzF:L3G+
K562 MWjDfZRwfG:6aXOgRZN{[Xl? NVvSPVVnQTZiaB?= NWnZOnJPTE2VTx?= NEf1TVZKSzVyPUKg{txO M{LYR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
DU145 Ml3yR5l1d3SxeHnjJGF{e2G7 MmftPVYhcA>? NEPLXYVFVVOR MnnFTWM2OD15LkWg{txO M3S0NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 Mk[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOxJO69VQ>? NX7DcHJ[OjRiaB?= M4DkVWROW09? M1vmdmNmdGxiY4njcIUh[XK{ZYP0JIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEBIOSCyaHHz[S=> NEnEOmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MCF7 M3u3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojtNUDPxE1? MkP1NlQhcA>? M4\rTGROW09? NFTqT|hE\WyuIHP5Z4xmKGG{cnXzeEBie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzFicHjhd4U> M1zMTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MCF7 M1PpSWtqdmG|ZTDBd5NigQ>? M3Tj[FUh|ryP NXK0PJZPOjRiaB?= MWrEUXNQ NGjyTYtKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JGNFUzRxY4njcIlvTDFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC{ZYTpco9jdGG|dH;tZUBxcG:|cHjvdplt[XSrb36gZZQhW2W{N{iw NEfqXZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MDA-MB-231 NHTPO3BMcW6jc3WgRZN{[Xl? NYnwWFVjPSEQvF2= MVWyOEBp NEG0fHpFVVOR MWDJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IFPET|Qw[3mlbHnuSFEh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBz\XSrbn;icIF{fG:vYTDwbI9{eGixconsZZRqd25iYYSgV4VzPzhy NVjScmhHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2PjZpPkK0OFE4PTZ4PD;hQi=>
MDA-MB-231 M4O0fmZ2dmO2aX;uJGF{e2G7 M4XDe|EuOTBizszN MWOyOEBp MVvEUXNQ NGD2dWRld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nzJIF{e2W|c3XkJIF{KFCDUmCgZ4xm[X[jZ3W= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 NVHSRYVZTnWwY4Tpc44hSXO|YYm= M4e4RVEuOTBizszN MmjWNlQhcA>? M{fGO2ROW09? NHzxT3dld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nzJIF{e2W|c3XkJIF{KFCDUmCgZ4xm[X[jZ3W= MoPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
MDA-MB-231 NWSzTG5WTnWwY4Tpc44hSXO|YYm= NEfO[poxNjVvMTFOwG0> MWW0PEBp NV3DNmNXTE2VTx?= M2HXR4hieyCwbzDD[YxtKGO7Y3zlJIFzemW|dDDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgd5VjNUdzIIDoZZNm MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 NVvSRVA4TnWwY4Tpc44hSXO|YYm= M3m2TFAvPS1zIN88US=> M2jzbVQ5KGh? NXrZWI5xTE2VTx?= M4PJN4hieyCwbzDD[YxtKGO7Y3zlJIFzemW|dDDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgd5VjNUdzIIDoZZNm M{fwOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MOLM13 NXfid5lnS0SNNDDpcohq[mm2aX;uJIF{e2G7 NYDjUGsyOjRiaB?= Mlv5TWM2OCB;IECuNFEyKM7:TR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
A2780 M{Toe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVu3NkBp NILURmNIUTVyIE2gNE4xOzJizszN Ml[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
COLO205 MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NX\j[2UyPzJiaB?= MmHOTWM2OCB;IECuNFM3KM7:TR?= MlvxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MV4-11 M2n0PWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\SO|IhcA>? NVHuSW5lT0l3MDC9JFAvODVizszN NEXWNms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
MOLM13 NXjHXZFpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH\BO3o4OiCq M2HQfWdKPTBiPTCwMlA3OiEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
NB4 M{fNbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWW3NkBp MXjHTVUxKD1iMD6wOlYh|ryP NVjYUGg6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
PC3 NHKwNXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1vHdlczKGh? NYrReVdJT0l3MDC9JFAvODdzIN88US=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
MOLM13 NYGyR|FUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NHfmWnM4OiCq NWm3fYNqUUN3MDC9JFAvODl4IN88US=> MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
MOLM13 MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M3O3VVczKGh? M2Dxb2lEPTBiPTCwMlA6PiEQvF2= NIq2RXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MDA-MB-453 NYXMNpYzS3m2b4TvfIlkcXS7IHHzd4F6 NXPaZY06PDhiaB?= NHThZ5RKSzVyIE2gNE4yOzdizszN NGK4RYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{S0PFkyOyd-Mke0OFg6OTN:L3G+
U937 MoK2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M13QS|czKGh? MWXJR|UxKD1iMD6xOEDPxE1? NYTyWo5DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MDA-MB-435 MmrXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M1ziZlI1KGh? M4Oy[WlEPTBiPTCwMlE3KM7:TR?= NYX3R2tqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVU2PzFpPkK2NVE2PTdzPD;hQi=>
MCF7 M2Hl[mN6fG:2b4jpZ4l1gSCjc4PhfS=> Mm\rOFghcA>? MWXJR|UxKD1iMD6yOEDPxE1? M1TIdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NES4PVE{Lz5{N{S0PFkyOzxxYU6=
MDA-MB-453 MlvmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUHacIJuPzJiaB?= NX;CTo5jT0l3MDC9JFAvOzJ4IN88US=> MmHNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
MCF7 NYP2NWQ6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFqxbWM4OiCq NHvMNIxIUTVyIE2gNE42PTdizszN NG[wdFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
MDA-MB-231 MWTDfZRwfG:6aXPpeJkh[XO|YYm= MmjsOFghcA>? NWr5XI1OUUN3MDC9JFAvPThizszN M4XnZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NES4PVE{Lz5{N{S0PFkyOzxxYU6=
M229 NIDj[JJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWm3NkBp MUHHTVUxKD1iMT6yNkDPxE1? NUmyOJd4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
M238 NFfneYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\SWHc4OiCq NWjlTJhlT0l3MDC9JFEvQTdizszN M3W2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
M249 NUH6UINwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{j3cFczKGh? NUHTW3NsT0l3MDC9JFEvQTlizszN M2rhfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
K562 NWDWNGpuS3m2b4TvfIlkcXS7IHHzd4F6 Mnr5PVYhcA>? NEfZdWhKSzVyIE2gNkDPxE1? MonVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
M249R NVPtUZFoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXe3NkBp MYXHTVUxKD1iMj65OkDPxE1? M2O0WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
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NCI-H1563 M2rLSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\UTWlEPTB;M{euNlQ5PCEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
DBTRG-05MG NEf1NlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvnTWM2OD1|OD6wOlkyKM7:TR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H630 NGWzU3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN6LkS3NVQh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H1155 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN7LkK0NkDPxE1? NUDBPHRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
OVACR-3 M1PlO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TEemlEPTB;M{muPVE6PSEQvF2= NF;FcnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
OAW-42 NHXkd5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULndm54UUN3ME20NE41OjV6IN88US=> NFHweXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
JVM-2 NIf2eHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO1VG51UUN3ME20NU4zPDF3IN88US=> Mn;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
C3A NHjDZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr3[nhxUUN3ME20NU4{PDR5IN88US=> MkLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
HT55 NUXlTG9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPNOIJKSzVyPUSyMlI5PDFizszN NVXHd4hNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
OVCAR-4 NEGxPVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFz1blZKSzVyPUSyMlI6PzRizszN MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
MEG-01 M3i5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Xp[mlEPTB;NEKuOFYyPiEQvF2= MmjBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
NCI-H82 Mnr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLxfppKSzVyPUSzMlk5QTJizszN MkTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
JEG-3 NV\QS4R4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTR2Lkm0O{DPxE1? NH3SNnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
BPH-1 MlLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{X6ZmlEPTB;NE[uN|k6QCEQvF2= NVHNWXZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
MPP-89 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m2VGlEPTB;NEeuNlg6QCEQvF2= NWD1cGdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ALL-PO MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;mXY17UUN3ME20O{41OTh6IN88US=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
HT NE\wU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLkTWM2OD12Nz60PVIh|ryP M3nXb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H2347 M4G2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTqW3pKSzVyPUS4MlA4OTVizszN M4rYZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
A2780 MkOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPqRocxUUN3ME20PU41OjJ6IN88US=> NIL0VWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
KARPAS-299 M4HOPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rKZmlEPTB;NEmuOVEyQSEQvF2= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H1651 NFvhdZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TDTmlEPTB;NEmuPFgzOSEQvF2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO; 

PubMed: 30300583     


Immunoblots showing dose-dependent impact of 72 hr palbociclib treatment on indicated protein levels in Kasumi-1 and SKNO-1 cells.

pRb(S807, 811) / CDK4 / CDK6 / PARP; 

PubMed: 28453226     


Effects of palbociclib on CDK4/6-Rb pathway. HCC cells were treated with different doses of palbociclib for 24 h, and then, the cells were subjected to western blot analysis. CF, cleaved fragment. 

LC3-I / LC3-II; 

PubMed: 28453226     


Palbociclib increases LC3-II amount in a dose-dependent manner in HCC cell lines. 

pAMPKα(T172) / pULK1(S317); 

PubMed: 28453226     


Dose-dependent response of palbociclib on AMPK-related molecules. HCC cells were treated with different concentrations of palbociclib for 24 h. The phosphorylation of the indicated proteins was determined by western blotting. 

SMAD2 (pS255); 

PubMed: 30343527     


T47D cells were treated with indicated concentrations of palbociclib for 24 h to evaluate substrate phosphorylation.

30300583 28453226 30343527
Growth inhibition assay
Cell viability; 

PubMed: 29670090     


Cell viability was determined by MTT assays after palbociclib exposure for 2, 4, and 6 days. The cell cycle of SYO-1 and Fuji cells was assessed after exposure to palbociclib (1 µM) for 24 h by flow cytometry analysis.

29670090
Immunofluorescence
SAHF/ATRX; 

PubMed: 26988987     


DAPI staining for senescence-associated heterochromatic foci (SAHF, left panel) and ATRX staining (right panel) in 1205Lu cells +/− palbociclib for 8 days. 

LC3B; 

PubMed: 28453226     


LC3B immunofluorescence in palbociclib‐treated Hep3B cells. Arrowheads indicate LC3-positive autophagosomes. Nuclei were counterstained with DAPI (blue).

26988987 28453226
ELISA
PGE2; 

PubMed: 26540629     


The supernatant of control and 7.5 μM palbociclib-treated cells was collected and stored at −80°C. PGE2 secretion was detected using ELISA.

26540629
体内研究 150 mg/kg PD 0332991处理 MDA-MB-435移植瘤完全抑制肿瘤。在多种人类肿瘤移植瘤中,PD 0332991也显示广谱抗癌活性,通过除去血管中p-Rb和增殖Marker Ki-67,且调节基因使其处于E2F转录水平控制。[1]

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)

激酶实验:

[1]

- 合并

Cdk实验:

PD0332991溶解在DMSO中。在96孔板上进行CDK 实验。通过杆状病毒感染,所有的CDK-cyclin 激酶复合体 在昆虫细胞中表达。实验底物为与GST融合的一段pRb。每孔体积为0.1 ml,包含:终浓度为20 mm Tris-HCl(pH 为7.4), 50 mmNaCl, 1 mm二硫苏糖醇, 10 mmMgCl2, 25 μm ATP (用于CDK4-cyclin D1, CDK6-cyclin D2,和CDK6-cyclin D3)或12 μm ATP (用于CDK2-cyclin E, CDK2-cyclin A, 和CDC2-cyclin B),0.25 μCi [γ-32P]ATP, 20 ng 酶, 1 μg GST·RB-Cterm, 及PD 0332991 (0.001-0.1μM)。除了[γ-32P]ATP的所有混合物加到孔中,放在搅拌器上搅拌2分钟。加入 [γ-32P]ATP开始反应, 在25 oC下温育15分钟。加入0.1 ml 20% 三氯乙酸终止反应, 在4 oC维持至少1小时,使底物沉淀。用0.2 ml 10%三氯乙酸冲洗5次,用β-计数器板测定掺入的放射性。
细胞实验:

[1]

- 合并
  • Cell lines: MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM,和K562细胞
  • Concentrations: 0.01-1 μM
  • Incubation Time: 24小时
  • Method:

    肿瘤细胞包括MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM,及K562按每孔2×104个细胞接种在96孔板上,温育过夜。加入PD 0332991 (0.01-1 μM) ,37oC温育24小时。每孔加入[14C]胸甘(0.1 μCi) ,进行同位素示踪,持续72小时。用β-计数器板测定掺入的放射性。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 携带晚期人类肿瘤移植瘤,包括结肠-205, MDA-MB-435 乳腺癌, SF-295 恶性胶质瘤, ZR-75-1 乳腺癌, PC-3 前列腺癌, H125 肺癌, SW-620结肠癌, H23肺癌,及MDA-MB-468 乳腺癌 (Rb 阴性)的SCID鼠
  • Dosages: 0-150 mg/kg
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 Water 30 mg/mL (61.98 mM)
DMSO 3 mg/mL warmed (6.19 mM)
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):
Saline
6 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 483.99
化学式

C24H29N7O2.HCl

CAS号 827022-32-2
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
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、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
NCT04841148 Not yet recruiting Drug: HCQ|Drug: Avelumab|Drug: Palbociclib Breast Cancer Abramson Cancer Center of the University of Pennsylvania|Johns Hopkins University|Translational Breast Cancer Research Consortium|Pfizer|Breast Cancer Research Foundation May 2021 Phase 2
NCT04669587 Recruiting Drug: ZB716|Drug: Palbociclib Estrogen Receptor-Positive|HER2-Negative|Locally Advanced Breast Cancer|Metastatic Breast Cancer EnhancedBio USA Inc.|Zenopharm LLC|EnhancedBio Inc. May 10 2021 Phase 1|Phase 2
NCT04735367 Not yet recruiting Drug: palbociclib plus letrozole Breast Cancer Pfizer February 1 2021 --
NCT04654208 Recruiting Drug: palbociclib Malignant Neoplasm of Breast Pfizer December 15 2020 --
NCT04671615 Recruiting Drug: palbociclib Metastatic Breast Cancer Pfizer December 6 2020 --

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

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID