Palbociclib (PD-0332991) HCl

For research use only.

Licensed by Pfizer Catalog No.S1116

286 publications

Palbociclib (PD-0332991) HCl Chemical Structure

CAS No. 827022-32-2

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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Selleck's Palbociclib (PD-0332991) HCl has been cited by 286 publications

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Choose Selective CDK Inhibitors

Biological Activity

Description Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Features Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Targets
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
In vitro

PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 μM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells. [1] PD 0332991 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. [2] PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. [3] A recent study shows that PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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MOLM13 NITOU4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX63NkBp MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTF2xN{Bk\WyuczDoZZJjd3KrbnegSmxVOyCLVFSgcZV1[W62IHHzd4V{e2WmIHHzJIlv[2:{cH;yZZRqd25ib3[gX|NJZXSqeX3p[Ilv\SCrboTvJGRPSSC5aYToJGlEPTBib3[gNE4xQTZizszN MnTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MOLM13 M3\YS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoO1O|IhcA>? M{TmU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sgd49z[W[nbnniMZJme2m|dHHueEBpfW2jbjDNU2xOOTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkC5OkDPxE1? NIqwVVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
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MDA-MB-231 M4fWTWZ2dmO2aX;uJGF{e2G7 MlW2NU0yOCEQvF2= MWeyOEBp NWHz[nlxTE2VTx?= MUPkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m|IHHzd4V{e2WmIHHzJHBCWlBiY3zlZZZi\2V? MkPpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
MCF7 Mn;4SpVv[3Srb36gRZN{[Xl? NYPUb4lxOS1zMDFOwG0> MXWyOEBp NIHZSpJFVVOR M1\IR4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYOgZZN{\XO|ZXSgZZMhWEGUUDDjcIVifmGpZR?= M1K3bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 M324[2Z2dmO2aX;uJGF{e2G7 M4frTFAvPS1zIN88US=> MmTiOFghcA>? NVfQSG9[TE2VTx?= M4fD[ohieyCwbzDD[YxtKGO7Y3zlJIFzemW|dDDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgd5VjNUdzIIDoZZNm MmLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
MCF7 NFzuc4VHfW6ldHnvckBCe3OjeR?= Mlj4NE42NTFizszN MWK0PEBp NGHWU2pFVVOR NXiwR|ZMcGG|IH7vJGNmdGxiY4njcIUh[XK{ZYP0JIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEB{fWJvR{GgdIhie2V? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MOLM13 NHHkfJpETEt2IHnubIljcXSrb36gZZN{[Xl? NXnJTVliOjRiaB?= M1XQZmlEPTBiPTCwMlAyOSEQvF2= NWDZV2JZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
A2780 Mkn1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmfUO|IhcA>? NGrKRYNIUTVyIE2gNE4xOzJizszN NXXVUHI3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
COLO205 M3X6dmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MUC3NkBp MnLYTWM2OCB;IECuNFM3KM7:TR?= MoLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MV4-11 NFzyVlhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvVZoZnPzJiaB?= NVnuNm04T0l3MDC9JFAvODVizszN MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
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MOLM13 MoTsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MVy3NkBp M37aeGlEPTBiPTCwMlA6PiEQvF2= NY\LWndZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
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MCF7 Ml3BR5l1d3SxeHnjbZR6KGG|c3H5 M1:x[FQ5KGh? NEXhWmRKSzVyIE2gNE4zPCEQvF2= NW\wbppJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0OFg6OTNpPkK3OFQ5QTF|PD;hQi=>
MDA-MB-453 MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYrNfnc3PzJiaB?= MlT5S2k2OCB;IECuN|I3KM7:TR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
MCF7 M2nP[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWXVOpZRPzJiaB?= NGT1Z|ZIUTVyIE2gNE42PTdizszN NELzVHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
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M229 MoPIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUC3NkBp MkfGS2k2OCB;IEGuNlIh|ryP NVe0XZZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
M238 M2i1VWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2qxT|czKGh? NWm3N5BiT0l3MDC9JFEvQTdizszN M1\0WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
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NCI-H630 NHi1[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\wRZlDUUN3ME2zPE41PzF2IN88US=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H1155 NGHGU3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHztb41KSzVyPUO5MlI1OiEQvF2= Mon1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
OVACR-3 MkL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvNOHdUUUN3ME2zPU46OTl3IN88US=> NIrsXnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
OAW-42 NIXCdFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTRyLkSyOVgh|ryP MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
JVM-2 MlnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTRzLkK0NVUh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
C3A MmfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL0UXpKSzVyPUSxMlM1PDdizszN NHWyZlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
HT55 M2DNTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TyWGlEPTB;NEKuNlg1OSEQvF2= M1n1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
OVCAR-4 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDMN3ZKSzVyPUSyMlI6PzRizszN MlzXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
MEG-01 NHXzVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\uNWo2UUN3ME20Nk41PjF4IN88US=> MnHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
NCI-H82 NHSwZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETGUHZKSzVyPUSzMlk5QTJizszN Ml;OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
JEG-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDqe3dKSzVyPUS0Mlk1PyEQvF2= NGfjfmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
BPH-1 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnOVFRQUUN3ME20Ok4{QTl6IN88US=> NUexeJJXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
MPP-89 NVPMOFJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\iZ2lEPTB;NEeuNlg6QCEQvF2= NYLvSZBYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ALL-PO NWPnRo5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTR5LkSxPFgh|ryP M4XzZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
HT M3HYUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrTdlhKSzVyPUS3MlQ6OiEQvF2= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H2347 NW\pWlhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nOcmlEPTB;NEiuNFcyPSEQvF2= MkflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
A2780 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLzeHNKSzVyPUS5MlQzOjhizszN NWjpSW1uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
KARPAS-299 M4\z[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j3NGlEPTB;NEmuOVEyQSEQvF2= MnPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
NCI-H1651 M4f1dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDUTWM2OD12OT64PFIyKM7:TR?= NFvtTY49[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
In vivo PD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F. [1]

Protocol

Kinase Assay:

[1]

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Cdk Assays:

A stock solution of PD0332991 is prepared in DMSO. CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and PD 0332991 (0.001-0.1μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25 °C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4  °C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.
Cell Research:

[1]

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  • Cell lines: Tumor cell lines including MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM and K562
  • Concentrations: 0.01-1 μM
  • Incubation Time: 24 hours
  • Method:

    Cells are seeded at 2 × 104 per well in a 96-well plate and incubated overnight. PD 0332991 (0.01-1 μM) is added to the wells and incubated at 37 °C for another 24 hours. [14C]Thymidine (0.1 μCi) is added to each well and incorporation of the radiolabel is allowed to proceed for 72 hours. Incorporated radioactivity is determined with a β plate counter.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Advanced stage human tumor xenografts including Colo-205, MDA-MB-435 breast, SF-295 glioblastoma, ZR-75-1 breast, PC-3 prostate, H125 lung, SW-620 colon, H23 lung and MDA-MB-468 breast (Rb negative) are established in severe combined immunodeficient mice.
  • Dosages: 0-150 mg/kg
  • Administration: Given by gavage
    (Only for Reference)

Solubility (25°C)

In vitro Water 30 mg/mL (61.98 mM)
DMSO 3 mg/mL warmed (6.19 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
6 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 483.99
Formula

C24H29N7O2.HCl

CAS No. 827022-32-2
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04669587 Not yet recruiting Drug: ZB716|Drug: Palbociclib Estrogen Receptor-Positive|HER2-Negative|Advanced|Metastatic Breast Cancer EnhancedBio USA Inc.|Zenopharm LLC|EnhancedBio Inc. February 1 2021 Phase 1|Phase 2
NCT04671615 Active not recruiting Drug: palbociclib Metastatic Breast Cancer Pfizer December 6 2020 --
NCT04567420 Not yet recruiting Drug: Palbociclib|Drug: Fulvestrant|Drug: Adjuvant Therapy Breast Cancer Criterium Inc. December 15 2020 Phase 2
NCT04654208 Not yet recruiting Drug: palbociclib Malignant Neoplasm of Breast Pfizer November 30 2020 --
NCT04483505 Recruiting Drug: Combination Rogaratinib + palbociclib + fulvestrant Breast Cancer Metastatic|Hormone Receptor Positive Malignant Neoplasm of Breast Fundacion CRIS de Investigación para Vencer el Cáncer|Bayer|Pfizer|Apices Soluciones S.L. November 25 2020 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID