Palbociclib (PD-0332991) HCl

For research use only.

Licensed by Pfizer Catalog No.S1116

299 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 299 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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U937 NFXtXFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDCfIY4OiCq NIfyWZNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMUSg{txO NIG4Z409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MOLM13 NXrv[HJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfrXoR[PzJiaB?= NXu3NWNHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTNiY3XscJMhcGG{Yn;ybY5oKE[OVEOgTXRFKG23dHHueEBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEm2JO69VQ>? MmnVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MOLM13 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjNcpc4OiCq M3;0XWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sgd49z[W[nbnniMZJme2m|dHHueEBpfW2jbjDNU2xOOTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkC5OkDPxE1? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
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MDA-MB-231 Ml3ESpVv[3Srb36gRZN{[Xl? NELhflgyNTFyIN88US=> M{jzcFI1KGh? MWHEUXNQ NELicHZld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nzJIF{e2W|c3XkJIF{KFCDUmCgZ4xm[X[jZ3W= NHjyW|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
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MDA-MB-231 MlT6SpVv[3Srb36gRZN{[Xl? MU[wMlUuOSEQvF2= NFv4eII1QCCq M3nseGROW09? M{nzZohieyCwbzDD[YxtKGO7Y3zlJIFzemW|dDDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgd5VjNUdzIIDoZZNm MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 Ml71SpVv[3Srb36gRZN{[Xl? MVuwMlUuOSEQvF2= MVi0PEBp NXjxbWZzTE2VTx?= NXjYdGFycGG|IH7vJGNmdGxiY4njcIUh[XK{ZYP0JIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEB{fWJvR{GgdIhie2V? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MOLM13 NFPhTo1ETEt2IHnubIljcXSrb36gZZN{[Xl? Moq0NlQhcA>? MkXBTWM2OCB;IECuNFEyKM7:TR?= NVjrNJp3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
A2780 NWDxcmV1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIrvOZc4OiCq NF\PUYVIUTVyIE2gNE4xOzJizszN NX7UPIlqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
COLO205 NVW3SplnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NVfaVIVpPzJiaB?= NWDpOnNiUUN3MDC9JFAvODN4IN88US=> MoLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MV4-11 M2rx[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXu3NkBp MkTFS2k2OCB;IECuNFUh|ryP NGj3S|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
MOLM13 MlqxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUD3c3JFPzJiaB?= MXvHTVUxKD1iMD6wOlIh|ryP NX3LPIJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
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MOLM13 MnjkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MXi3NkBp MVHJR|UxKD1iMD6wPVYh|ryP NGXWXVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MOLM13 NGq2[pFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MojIO|IhcA>? M4nvOmlEPTBiPTCwMlA6PiEQvF2= NVnid4M2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
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MDA-MB-453 MlrSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjXZlQ4OiCq MXnHTVUxKD1iMD6zNlYh|ryP NIfKW3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
MCF7 NGLoc5ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHXsW2U4OiCq MXnHTVUxKD1iMD61OVch|ryP NHLIWXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
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BALL-1 NEjaRYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnqXGlXUUN3ME2yOk46Ozl5IN88US=> NXXtOHZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
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NCI-H630 M3WyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrMTW5KSzVyPUO4MlQ4OTRizszN M3PYbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H1155 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\jTmlEPTB;M{muNlQzKM7:TR?= NVfrRlZvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
OVACR-3 NYLTU5A6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MliwTWM2OD1|OT65NVk2KM7:TR?= M1zBRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
OAW-42 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;RTWM2OD12MD60NlU5KM7:TR?= Ml\2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
JVM-2 NV3GWItuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Tw[GlEPTB;NEGuNlQyPSEQvF2= NXeyfnBQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
C3A MmfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL2TWM2OD12MT6zOFQ4KM7:TR?= M2XE[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
HT55 M3XaV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTR{LkK4OFEh|ryP M3fhNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
OVCAR-4 NXTQWXBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3qTWM2OD12Mj6yPVc1KM7:TR?= NW\vcm9MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
MEG-01 NG[yUZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D3V2lEPTB;NEKuOFYyPiEQvF2= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H82 M2fSVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTR|Lkm4PVIh|ryP M{X6ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
JEG-3 MlfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ezd2lEPTB;NESuPVQ4KM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
BPH-1 M{XPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;NTWM2OD12Nj6zPVk5KM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
MPP-89 M1fCbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XsTGlEPTB;NEeuNlg6QCEQvF2= NX;kRVZCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ALL-PO NWm2bZZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLrOGhKSzVyPUS3MlQyQDhizszN NEPzTo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
HT NFP3d3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPKTWM2OD12Nz60PVIh|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NCI-H2347 NGjsNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLSTWM2OD12OD6wO|E2KM7:TR?= NUTEcWR[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
A2780 NGjEOVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPKXm5KSzVyPUS5MlQzOjhizszN MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
KARPAS-299 MlLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTR7LkWxNVkh|ryP M3fxPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H1651 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTR7Lki4NlEh|ryP MWq8ZUB1[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
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
CalculateReset

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
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 --

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