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307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 NIjYRlNMcW6jc3WgRZN{[Xl? MmH4NlQhcA>? MWXJcohq[mm2aX;uJI9nKEOGS{SgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDSZkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMECyJO69VQ>? M3fQe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
COLO205 NWPPVY1xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHme4g4OiCq NGrpV|ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEO2JO69VQ>? NF3tVVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
U937 M4rwd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[wclczKGh? MlG4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6lb4Lwc5JifGmxbjDv[kBcO0ifdHj5cYllcW6nIHnueI8hTE6DIIfpeIghUUN3MDDv[kAxNjF2IN88US=> NH7lWXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MOLM13 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjPPGQ4OiCq MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTF2xN{Bk\WyuczDoZZJjd3KrbnegSmxVOyCLVFSgcZV1[W62IHHzd4V{e2WmIHHzJIlv[2:{cH;yZZRqd25ib3[gX|NJZXSqeX3p[Ilv\SCrboTvJGRPSSC5aYToJGlEPTBib3[gNE4xQTZizszN NGPuPXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MOLM13 NGjHT4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnP3O|IhcA>? NIDjVVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JJNwemGoZX7pZk1z\XOrc4ThcpQhcHWvYX6gUW9NVTF|IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ49zeG:{YYTpc44hd2ZiW{PIYZRpgW2rZHnu[UBqdnSxIFTORUB4cXSqIFnDOVAhd2ZiMD6wPVYh|ryP NWfZbIxKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MDA-MB-435 NILiTIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;NXFBpOjRiaB?= MVXJR|UxRTBwMU[g{txO NX\yfWpwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4NFE5OzFpPkG1PFAyQDNzPD;hQi=>
K562 NW\0NGs2S3m2b4TvfIlkKEG|c3H5 NXi1UJJIQTZiaB?= NHjGem9FVVOR MnvSTWM2OD1{IN88US=> NUPNc4FsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2PjZpPkK0OFE4PTZ4PD;hQi=>
DU145 MXXDfZRwfG:6aXOgRZN{[Xl? NIe5VHM6PiCq MXXEUXNQ M4DudWlEPTB;Nz61JO69VQ>? M3LnXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnEUnUyKM7:TR?= M2jDW|I1KGh? Mk\BSG1UVw>? NH;LPYZE\WyuIHP5Z4xmKGG{cnXzeEBie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzFicHjhd4U> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2S3ZVEh|ryP MmTZNlQhcA>? NEjJc4VFVVOR NYPaSnh1S2WubDDjfYNt\SCjcoLld5Qh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdzIIDoZZNm MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 NVrZWppJU2mwYYPlJGF{e2G7 M4rwSVUh|ryP M4XXZVI1KGh? MV3EUXNQ M3j3dWlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgR2RMPC:leXPsbY5FOSCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKndHnuc4Jt[XO2b33hJJBpd3OyaH;yfYxifGmxbjDheEBU\XJ5OEC= M1\wPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 M2TMU2tqdmG|ZTDBd5NigQ>? M1TaUlUh|ryP NX3hZ|I2OjRiaB?= NGPCeVRFVVOR NYK1UYZpUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBETEt2L3P5Z4xqdkRzIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZicnX0bY5w[myjc4TvcYEheGixc4Doc5J6dGG2aX;uJIF1KFOncke4NC=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MDA-MB-231 MVfGeY5kfGmxbjDBd5NigQ>? M3:4WFEuOTBizszN NITQS2wzPCCq NWfpZ3M2TE2VTx?= MVrkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m|IHHzd4V{e2WmIHHzJHBCWlBiY3zlZZZi\2V? NUPzTVJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2PjZpPkK0OFE4PTZ4PD;hQi=>
MCF7 NHfsdo5HfW6ldHnvckBCe3OjeR?= NUfwTmI1OS1zMDFOwG0> M{[2TFI1KGh? MX7EUXNQ MXrkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m|IHHzd4V{e2WmIHHzJHBCWlBiY3zlZZZi\2V? NHXVPI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MDA-MB-231 MmewSpVv[3Srb36gRZN{[Xl? NELYbpAxNjVvMTFOwG0> M4PLcVQ5KGh? M2rUXmROW09? NFS0Rmhp[XNibn:gR4VtdCCleXPs[UBienKnc4SgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIHH0JJN2[i2JMTDwbIF{\Q>? M{fMblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MCF7 MWLGeY5kfGmxbjDBd5NigQ>? NW\wcmVMOC53LUGg{txO NHjScXo1QCCq MV7EUXNQ NEDWOYdp[XNibn:gR4VtdCCleXPs[UBienKnc4SgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIHH0JJN2[i2JMTDwbIF{\Q>? NFfFOWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MOLM13 M2e0TmNFUzRiaX7obYJqfGmxbjDhd5NigQ>? MXiyOEBp Mo\1TWM2OCB;IECuNFEyKM7:TR?= M1PqPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
A2780 M4nOSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NILSbHg4OiCq M4LqUGdKPTBiPTCwMlA{OiEQvF2= NELPNmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
COLO205 NY\hdFJlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MVe3NkBp MlfBTWM2OCB;IECuNFM3KM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
MV4-11 Mlz5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIe5W|Y4OiCq MorJS2k2OCB;IECuNFUh|ryP NHHkVW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
MOLM13 NWf3dIZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXO3NkBp NWe3S2U{T0l3MDC9JFAvODZ{IN88US=> M1f5OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
NB4 NYnkdHoxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVW3NkBp NH;TXXFIUTVyIE2gNE4xPjZizszN NIPmdlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
PC3 MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYXZVlJGPzJiaB?= MYrHTVUxKD1iMD6wO|Eh|ryP M2PWS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
MOLM13 M1XrNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NVKy[|NWPzJiaB?= NV\uVHZ5UUN3MDC9JFAvODl4IN88US=> MoDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MOLM13 Mlv6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MXe3NkBp MYLJR|UxKD1iMD6wPVYh|ryP NWjVN41{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MDA-MB-453 NHfwbXREgXSxdH;4bYNqfHliYYPzZZk> NVzMUIJEPDhiaB?= MmX6TWM2OCB;IECuNVM4KM7:TR?= NHnXVVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{S0PFkyOyd-Mke0OFg6OTN:L3G+
U937 MkLNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NUHVR2I3PzJiaB?= M1rIXmlEPTBiPTCwMlE1KM7:TR?= Mly1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MDA-MB-435 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M2TWb|I1KGh? NFfPXmVKSzVyIE2gNE4yPiEQvF2= NUWx[3FMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVU2PzFpPkK2NVE2PTdzPD;hQi=>
MCF7 NUTMSnZ6S3m2b4TvfIlkcXS7IHHzd4F6 MnzPOFghcA>? NXLZdllYUUN3MDC9JFAvOjRizszN NXX4cINbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0OFg6OTNpPkK3OFQ5QTF|PD;hQi=>
MDA-MB-453 NXyyR49jT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2ftWlczKGh? NVrGOYJtT0l3MDC9JFAvOzJ4IN88US=> MlTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
MCF7 NF76cW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fXd|czKGh? MVPHTVUxKD1iMD61OVch|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
MDA-MB-231 MmPjR5l1d3SxeHnjbZR6KGG|c3H5 M17t[lQ5KGh? MoLXTWM2OCB;IECuOVgh|ryP M4fwbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NES4PVE{Lz5{N{S0PFkyOzxxYU6=
M229 NXv1SIJJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4PVRVczKGh? MXnHTVUxKD1iMT6yNkDPxE1? MonUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
M238 NGjQNW1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M17JTlczKGh? MmTPS2k2OCB;IEGuPVch|ryP Mn\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
M249 MnfSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHPveWY4OiCq MkW2S2k2OCB;IEGuPVkh|ryP NXrp[XMzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
K562 NEjZUllEgXSxdH;4bYNqfHliYYPzZZk> NITmV5Q6PiCq NIG0S5BKSzVyIE2gNkDPxE1? M{\hZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
M249R M3W5R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M336c|czKGh? M1vZeWdKPTBiPTCyMlk3KM7:TR?= Mm\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
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NCI-H1563 NGewfYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jIZ2lEPTB;M{euNlQ5PCEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
DBTRG-05MG MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjTR3FwUUN3ME2zPE4xPjlzIN88US=> NFq2XVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
NCI-H630 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTXTWM2OD1|OD60O|E1KM7:TR?= NU\EfW5JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
NCI-H1155 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoW0TWM2OD1|OT6yOFIh|ryP Ml2zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
OVACR-3 NELE[3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDEW2tKSzVyPUO5MlkyQTVizszN NYXWSYNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
OAW-42 NYL2ZmJwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTRyLkSyOVgh|ryP MmHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
JVM-2 M2CwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTRzLkK0NVUh|ryP MojkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
C3A NUnDb3hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES0VIhKSzVyPUSxMlM1PDdizszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
HT55 NYH2WXZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j5OWlEPTB;NEKuNlg1OSEQvF2= M33Q[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
OVCAR-4 NUPZ[Jh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTPNY1jUUN3ME20Nk4zQTd2IN88US=> NVjhcXI2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
MEG-01 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m3NWlEPTB;NEKuOFYyPiEQvF2= M2nsXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H82 M1f6cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LNVWlEPTB;NEOuPVg6OiEQvF2= NHO5Roo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
JEG-3 Mom3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTR2Lkm0O{DPxE1? M2Hr[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
BPH-1 NXHSbXRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[0bIlHUUN3ME20Ok4{QTl6IN88US=> NHXlbpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
MPP-89 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrH[Y5KSzVyPUS3MlI5QThizszN NVPHcJFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ALL-PO M1L3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:yTWM2OD12Nz60NVg5KM7:TR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
HT Ml3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrucHJOUUN3ME20O{41QTJizszN MkXvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
NCI-H2347 NVvI[IU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIruSm1KSzVyPUS4MlA4OTVizszN MkPZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
A2780 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzQV4pKSzVyPUS5MlQzOjhizszN Ml;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
KARPAS-299 NX:w[IE2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX1OGhKSzVyPUS5MlUyOTlizszN MmW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
NCI-H1651 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr0VmtKSzVyPUS5Mlg5OjFizszN NFfFWG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,

... 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、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
NCT04669587 Recruiting Drug: ZB716|Drug: Palbociclib Estrogen Receptor-Positive|HER2-Negative|Locally Advanced Breast Cancer|Metastatic Breast Cancer EnhancedBio USA Inc.|Zenopharm|EnhancedBio Inc. July 26 2021 Phase 1|Phase 2
NCT04841148 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 June 1 2021 Phase 2

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