Palbociclib (PD-0332991) HCl

Licensed by Pfizer Catalog No.S1116

For research use only.

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.

Palbociclib (PD-0332991) HCl Chemical Structure

CAS No. 827022-32-2

Selleck's Palbociclib (PD-0332991) HCl has been cited by 351 publications

Purity & Quality Control

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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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COLO205 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmC0O|IhcA>? NV;telBzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkCzOkDPxE1? Mlr0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
U937 MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfFO|IhcA>? NHPXbpNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMUSg{txO MluzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MOLM13 MlXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jLOFczKGh? NGjYcIVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yOyClZXzsd{Bp[XKkb4LpcochTkyWMzDJWGQhdXW2YX70JIF{e2W|c3XkJIF{KGmwY3;ydI9z[XSrb36gc4YhYzOKXYTofY1q\GmwZTDpcpRwKESQQTD3bZRpKEmFNUCgc4YhOC5yOU[g{txO MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
MOLM13 NHTtUWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzMSXY4OiCq NGG3VXBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JJNwemGoZX7pZk1z\XOrc4ThcpQhcHWvYX6gUW9NVTF|IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ49zeG:{YYTpc44hd2ZiW{PIYZRpgW2rZHnu[UBqdnSxIFTORUB4cXSqIFnDOVAhd2ZiMD6wPVYh|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
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K562 MmX0R5l1d3SxeHnjJGF{e2G7 MkjnPVYhcA>? NGXE[4pFVVOR MYrJR|UxRTJizszN NXLPdmFIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2PjZpPkK0OFE4PTZ4PD;hQi=>
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MCF7 NWmwXG9ZU2mwYYPlJGF{e2G7 M{DGTFUh|ryP MUGyOEBp MlfoSG1UVw>? Ml\jTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDDSGs1N2O7Y3zpcmQyKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhemW2aX7vZoxie3SxbXGgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmejd6MB?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
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MDA-MB-231 MULGeY5kfGmxbjDBd5NigQ>? MkD4NU0yOCEQvF2= MmjqNlQhcA>? NUHZV4JjTE2VTx?= NGHiPIlld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nzJIF{e2W|c3XkJIF{KFCDUmCgZ4xm[X[jZ3W= M2G5NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MCF7 MVfGeY5kfGmxbjDBd5NigQ>? MWexMVExKM7:TR?= MoLENlQhcA>? MmK4SG1UVw>? NILIT4pld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nzJIF{e2W|c3XkJIF{KFCDUmCgZ4xm[X[jZ3W= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MDA-MB-231 MnfGSpVv[3Srb36gRZN{[Xl? NV3DXmJqOC53LUGg{txO MlfiOFghcA>? NWPhbIdbTE2VTx?= M2nJbIhieyCwbzDD[YxtKGO7Y3zlJIFzemW|dDDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgd5VjNUdzIIDoZZNm NWHBbZk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2PjZpPkK0OFE4PTZ4PD;hQi=>
MCF7 MWDGeY5kfGmxbjDBd5NigQ>? NH;wdW4xNjVvMTFOwG0> MoLrOFghcA>? MVfEUXNQ MVzoZZMhdm9iQ3XscEBkgWOuZTDhdpJme3RiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IIP1Zk1IOSCyaHHz[S=> NIixO|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MOLM13 MoL0R2RMPCCrbnjpZol1cW:wIHHzd4F6 MofsNlQhcA>? MXHJR|UxKD1iMD6wNVEh|ryP MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
A2780 M3;kZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnLkO|IhcA>? NWj2N5VNT0l3MDC9JFAvODN{IN88US=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
COLO205 NIPqPZlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NIPhdIo4OiCq M4LIXWlEPTBiPTCwMlA{PiEQvF2= NWXyZ2dNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MV4-11 MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2j0bVczKGh? M3TPdGdKPTBiPTCwMlA2KM7:TR?= Mn3HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
MOLM13 Ml;FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWG3NkBp M2PRSWdKPTBiPTCwMlA3OiEQvF2= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
NB4 NH\IcINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4P6SFczKGh? NVHO[YJGT0l3MDC9JFAvODZ4IN88US=> M4rZWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
PC3 NIjZUZZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoHvO|IhcA>? M1SzdWdKPTBiPTCwMlA4OSEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
MOLM13 MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NIXZOWs4OiCq NFy0T|RKSzVyIE2gNE4xQTZizszN Mn3YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MOLM13 M4C1W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M37YeFczKGh? M4HpT2lEPTBiPTCwMlA6PiEQvF2= NWLJdZF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MDA-MB-453 Mn[2R5l1d3SxeHnjbZR6KGG|c3H5 M2fDWFQ5KGh? MYTJR|UxKD1iMD6xN|ch|ryP MmXEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd2NEi5NVMoRjJ5NES4PVE{RC:jPh?=
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MCF7 NY\VNXJRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1P4[|czKGh? MYnHTVUxKD1iMD61OVch|ryP M4LzUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
MDA-MB-231 Ml2yR5l1d3SxeHnjbZR6KGG|c3H5 NYezb3NJPDhiaB?= NXHOeHFiUUN3MDC9JFAvPThizszN MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR2OEmxN{c,Ojd2NEi5NVM9N2F-
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M249 Mk\ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF2yZYk4OiCq NXfGb4lVT0l3MDC9JFEvQTlizszN NV7SUII6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
K562 NYOxS2FkS3m2b4TvfIlkcXS7IHHzd4F6 NV\XS4dvQTZiaB?= NX7nfGREUUN3MDC9JFIh|ryP Ml3mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
M249R Ml;lS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1jYRVczKGh? MonOS2k2OCB;IEKuPVYh|ryP NUm3UmFURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
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MDA-MB-468 MlLSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NEXDTogzPCCq NWTJZ5Y1UUN3MDC9JFMh|ryP Ml3JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMUW1O|EoRjJ4MUG1OVcyRC:jPh?=
C4-2B MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjSO|IhcA>? NGX1c5pIUTVyIE2gOE4yPSEQvF2= MlniQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzNU[xNVEoRjJ6MUW2NVEyRC:jPh?=
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NCI-H630 Mlv3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v4SGlEPTB;M{iuOFcyPCEQvF2= MojmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
NCI-H1155 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjmcnBiUUN3ME2zPU4zPDJizszN M3nqXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
OVACR-3 NHHNfnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7LTWM2OD1|OT65NVk2KM7:TR?= M3TLXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
OAW-42 NWTEVXhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTRyLkSyOVgh|ryP NYW5UmV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
JVM-2 NYKwfVE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXsTWM2OD12MT6yOFE2KM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
C3A Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTRzLkO0OFch|ryP NYSwXJlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
HT55 NUiyeVhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonlTWM2OD12Mj6yPFQyKM7:TR?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
OVCAR-4 M{TkZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTR{LkK5O|Qh|ryP NH\EU|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
MEG-01 NYnG[5I4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjBWpRlUUN3ME20Nk41PjF4IN88US=> M37uSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H82 M2fxO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4H5PGlEPTB;NEOuPVg6OiEQvF2= MmrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
JEG-3 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Pyb2lEPTB;NESuPVQ4KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
BPH-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTR4LkO5PVgh|ryP M4nq[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
MPP-89 M4rTS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnsTWM2OD12Nz6yPFk5KM7:TR?= NWHtOFJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ALL-PO NHLwSnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PyOGlEPTB;NEeuOFE5QCEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
HT MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\uOGJKSzVyPUS3MlQ6OiEQvF2= M1;VcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H2347 NIXyc5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPk[XJ5UUN3ME20PE4xPzF3IN88US=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
A2780 MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;nbYlKSzVyPUS5MlQzOjhizszN M3exZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
KARPAS-299 NVG4Zmd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPTTWM2OD12OT61NVE6KM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H1651 NVnjfINDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[wbnJoUUN3ME20PU45QDJzIN88US=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
Assay
Methods Test Index PMID
Western blot RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO ; pRb(S807, 811) / CDK4 / CDK6 / PARP ; LC3-I / LC3-II ; pAMPKα(T172) / pULK1(S317) ; SMAD2 (pS255) 30300583 28453226 30343527
Growth inhibition assay Cell viability 29670090
Immunofluorescence SAHF/ATRX ; LC3B 26988987 28453226
ELISA PGE2 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

Water 30 mg/mL warmed
(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

Chemical Information

Molecular Weight 483.99
Formula

C24H29N7O2.HCl

CAS No. 827022-32-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05135104 Not yet recruiting Drug: Palbociclib Metastatic Breast Cancer Asociatia Oncohelp - Centrul de Oncologie Oncohelp|MDX Research November 15 2021 --
NCT05069038 Not yet recruiting Drug: Palbociclib 125mg Breast Cancer Jairam Krishnamurthy|University of Nebraska November 1 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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