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 361 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
MOLM13 NHnn[HlMcW6jc3WgRZN{[Xl? MWKyOEBp NGqzRndKdmirYnn0bY9vKG:oIFPET|Qh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBT[iCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFAzKM7:TR?= MoS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
COLO205 NETCW2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWK3NkBp NHjwfopCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEO2JO69VQ>? M2n0[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
U937 Mlm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHiwUIE4OiCq NU\LblRHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|ZYPz[YQh[XNiaX7jc5Jxd3KjdHnvckBw\iCdM1jdeIh6dWmmaX7lJIlvfG9iRF7BJJdqfGhiSVO1NEBw\iByLkG0JO69VQ>? M3zXVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
MOLM13 NXrFT3R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDKZY1ZPzJiaB?= NXP4bYVkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTNiY3XscJMhcGG{Yn;ybY5oKE[OVEOgTXRFKG23dHHueEBie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEm2JO69VQ>? NGeyfVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MOLM13 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPNS2FEPzJiaB?= MkDMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDzc5Ji\mWwaXKtdoV{cXO2YX70JIh2dWGwIF3PUG0yOyClZXzsd{Bie3Onc4Pl[EBieyCrbnPvdpBwemG2aX;uJI9nKFt|SG30bJlucWSrbnWgbY51dyCGTlGge4l1cCCLQ{WwJI9nKDBwMEm2JO69VQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
MDA-MB-435 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DqelI1KGh? MkP2TWM2OD1yLkG2JO69VQ>? NXHoWoJnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW4NFE5OzFpPkG1PFAyQDNzPD;hQi=>
K562 NUPJblYxS3m2b4TvfIlkKEG|c3H5 M2n1Z|k3KGh? M3S1emROW09? MWrJR|UxRTJizszN MoXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
DU145 NVLOTFFlS3m2b4TvfIlkKEG|c3H5 M{PGdFk3KGh? M1jhTWROW09? MniyTWM2OD15LkWg{txO M{mwTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWOxJO69VQ>? NGr2RXczPCCq NYfkZVB1TE2VTx?= NGnaZ4FE\WyuIHP5Z4xmKGG{cnXzeEBie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzFicHjhd4U> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 NFHCVlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmydYJJOSEQvF2= NYLaOWhwOjRiaB?= MlKxSG1UVw>? NULPOFdMS2WubDDjfYNt\SCjcoLld5Qh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdzIIDoZZNm MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
MCF7 NWrxSW5nU2mwYYPlJGF{e2G7 MYe1JO69VQ>? MmnyNlQhcA>? MYDEUXNQ NVP4bY1HUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBETEt2L3P5Z4xqdkRzIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZicnX0bY5w[myjc4TvcYEheGixc4Doc5J6dGG2aX;uJIF1KFOncke4NC=> M33mdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVY3Lz5{NESxO|U3PjxxYU6=
MDA-MB-231 NH7neFBMcW6jc3WgRZN{[Xl? MlmyOUDPxE1? MnrpNlQhcA>? Mnv1SG1UVw>? M4nFVGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgR2RMPC:leXPsbY5FOSCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHKndHnuc4Jt[XO2b33hJJBpd3OyaH;yfYxifGmxbjDheEBU\XJ5OEC= MljVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
MDA-MB-231 NXHuOWkzTnWwY4Tpc44hSXO|YYm= MV2xMVExKM7:TR?= NEWzRlYzPCCq NFuzZ3NFVVOR Ml3M[I9meyCwb4SgbY5lfWOnIHHwc5B1d3OrczDhd5Nme3OnZDDhd{BRSVKSIHPs[YF3[Wen MoLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
MCF7 MmDVSpVv[3Srb36gRZN{[Xl? NXnKV2JMOS1zMDFOwG0> M4HIfVI1KGh? MlntSG1UVw>? MXTkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m|IHHzd4V{e2WmIHHzJHBCWlBiY3zlZZZi\2V? Mlj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1OlYoRjJ2NEG3OVY3RC:jPh?=
MDA-MB-231 MYnGeY5kfGmxbjDBd5NigQ>? MVmwMlUuOSEQvF2= M3W3[FQ5KGh? NHrhSlhFVVOR NYTpSXd7cGG|IH7vJGNmdGxiY4njcIUh[XK{ZYP0JIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEB{fWJvR{GgdIhie2V? NInNfHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MCF7 NE\NfVdHfW6ldHnvckBCe3OjeR?= MYqwMlUuOSEQvF2= M4jsSFQ5KGh? MVfEUXNQ MnuwbIF{KG6xIFPlcIwh[3mlbHWgZZJz\XO2IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDzeYIuTzFicHjhd4U> NIS1cJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U3Pid-MkS0NVc2PjZ:L3G+
MOLM13 NFP5R4tETEt2IHnubIljcXSrb36gZZN{[Xl? MV6yOEBp MV;JR|UxKD1iMD6wNVEh|ryP NGW1S3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
A2780 MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWK3NkBp Mo[5S2k2OCB;IECuNFMzKM7:TR?= M3f1SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
COLO205 NF3GZWxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MYi3NkBp MX3JR|UxKD1iMD6wN|Yh|ryP NELUU5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[0NVExOyd-MkS2OFEyODN:L3G+
MV4-11 MkjqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWjESIF4PzJiaB?= NUPmfVlVT0l3MDC9JFAvODVizszN M3HaRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
MOLM13 MkPRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmP5O|IhcA>? NX\EcXBjT0l3MDC9JFAvODZ{IN88US=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
NB4 NFjSd5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIHPO204OiCq NF[4UINIUTVyIE2gNE4xPjZizszN M364R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
PC3 MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmrVO|IhcA>? MX7HTVUxKD1iMD6wO|Eh|ryP MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF3NkGxNUc,OjhzNU[xNVE9N2F-
MOLM13 M1PhNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M3\HdVczKGh? MX;JR|UxKD1iMD6wPVYh|ryP M{XLb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkSxNVA{Lz5{NE[0NVExOzxxYU6=
MOLM13 M3;NNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NHnw[VU4OiCq M3myWWlEPTBiPTCwMlA6PiEQvF2= MmfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NEGxNFMoRjJ2NkSxNVA{RC:jPh?=
MDA-MB-453 NHTNVJlEgXSxdH;4bYNqfHliYYPzZZk> MXm0PEBp M3XP[mlEPTBiPTCwMlE{PyEQvF2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR2OEmxN{c,Ojd2NEi5NVM9N2F-
U937 NFyzdWRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M4TON|czKGh? NWq0UlMyUUN3MDC9JFAvOTRizszN MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ2MUGwN{c,OjR4NEGxNFM9N2F-
MDA-MB-435 NXS4WYs4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NV;2RmZYOjRiaB?= NXHTXFlVUUN3MDC9JFAvOTZizszN NIfOZVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOVU4OSd-Mk[xNVU2PzF:L3G+
MCF7 NITwSWhEgXSxdH;4bYNqfHliYYPzZZk> NHf1d|U1QCCq MYHJR|UxKD1iMD6yOEDPxE1? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR2OEmxN{c,Ojd2NEi5NVM9N2F-
MDA-MB-453 M2HRd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGKyWVI4OiCq NV;Sb2tOT0l3MDC9JFAvOzJ4IN88US=> NV[3ZVZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
MCF7 MnHmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3LKeFczKGh? NXrO[Y57T0l3MDC9JFAvPTV5IN88US=> NYO5RnE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
MDA-MB-231 Mlm4R5l1d3SxeHnjbZR6KGG|c3H5 MWi0PEBp NGPPeGlKSzVyIE2gNE42QCEQvF2= NXn3S|JxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0OFg6OTNpPkK3OFQ5QTF|PD;hQi=>
M229 MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV;uVZRUPzJiaB?= NGP0d2lIUTVyIE2gNU4zOiEQvF2= NFfYcYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG1OlEyOSd-MkixOVYyOTF:L3G+
M238 NEPjdXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV24c3luPzJiaB?= NFHjXllIUTVyIE2gNU46PyEQvF2= NX72VmJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
M249 M3Ljbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVq3NkBp M1jwdmdKPTBiPTCxMlk6KM7:TR?= NYXQfIs2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
K562 NIXKS3JEgXSxdH;4bYNqfHliYYPzZZk> MmruPVYhcA>? NV\2cZZwUUN3MDC9JFIh|ryP MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{W2Okc,OjR2MUe1OlY9N2F-
M249R M1fERmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{n5cVczKGh? M2XQcGdKPTBiPTCyMlk3KM7:TR?= M33BOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUW2NVEyLz5{OEG1OlEyOTxxYU6=
MOLM13 Ml70SmxVOyCrbnjpZol1cW:wIHHzd4F6 NEnrUpUzPCCq NHPSfWpKSzVyIE2gN{DPxE1? NWXQSXdoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OFEyODNpPkK0OlQyOTB|PD;hQi=>
MDA-MB-468 MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NGS1TpEzPCCq M2jpT2lEPTBiPTCzJO69VQ>? NF\MVZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOVU4OSd-Mk[xNVU2PzF:L3G+
C4-2B MoXuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFPKUWY4OiCq NFrLSWtIUTVyIE2gOE4yPSEQvF2= NV3XNXd4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixOVYyOTFpPkK4NVU3OTFzPD;hQi=>
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NCI-H1155 M1\WO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TkVGlEPTB;M{muNlQzKM7:TR?= NYXNT5k1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
OVACR-3 NUTnR3o5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTtVXQ4UUN3ME2zPU46OTl3IN88US=> NGruUY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
OAW-42 M{XPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTRyLkSyOVgh|ryP M{W4O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
JVM-2 MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTRzLkK0NVUh|ryP NWTzeYs3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
C3A M4jzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHITWM2OD12MT6zOFQ4KM7:TR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
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OVCAR-4 M3XCb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTQS3RlUUN3ME20Nk4zQTd2IN88US=> M{\ROlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
MEG-01 Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PrWGlEPTB;NEKuOFYyPiEQvF2= NWS3OG05RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
NCI-H82 NUPZXWczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnrN2FKSzVyPUSzMlk5QTJizszN MkfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
JEG-3 NHnGOGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTvPGk6UUN3ME20OE46PDdizszN M2WwdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
BPH-1 MlrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDyTWM2OD12Nj6zPVk5KM7:TR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
MPP-89 M2P4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXES49NUUN3ME20O{4zQDl6IN88US=> NUW5SGpRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ALL-PO NUPNWY1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHP1WIVKSzVyPUS3MlQyQDhizszN NG\6TWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
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NCI-H2347 NFHnSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm5TWM2OD12OD6wO|E2KM7:TR?= NXnoNZFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
A2780 NVnLT3Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnzeVVKSzVyPUS5MlQzOjhizszN M2\FPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
KARPAS-299 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvRTWM2OD12OT61NVE6KM7:TR?= NGjaNJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
NCI-H1651 NV7qWYNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLZTWM2OD12OT64PFIyKM7:TR?= M4XWVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
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

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)

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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
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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
NCT05399329 Not yet recruiting Drug: Palbociclib|Drug: Endocrine therapy Breast Cancer Pfizer June 15 2022 --
NCT05293964 Recruiting Drug: SCR-6852|Drug: Palbociclib Breast Cancer Jiangsu Simcere Pharmaceutical Co. Ltd. May 18 2022 Phase 1
NCT05371275 Active not recruiting Drug: Palbociclib COVID-19 biotx.ai GmbH April 21 2022 Phase 2
NCT05069038 Recruiting Drug: Palbociclib 125mg Breast Cancer Jairam Krishnamurthy|University of Nebraska March 2 2022 Phase 2
NCT05452798 Active not recruiting -- Breast Cancer Pfizer February 24 2022 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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