Palbociclib (PD0332991) Isethionate

For research use only.

Licensed and Manufactured by Pfizer Catalog No.S1579

188 publications

Palbociclib (PD0332991) Isethionate Chemical Structure

CAS No. 827022-33-3

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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Selleck's Palbociclib (PD0332991) Isethionate has been cited by 188 publications

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Biological Activity

Description Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
Features The 1st specific inhibitor for CDK4/6 to show promise in multiple 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 exhibits absolute selectivity for CDK4/6 with little or no activity against other CDKs. PD 0332991 is effective at reducing Rb phosphorylation at Ser780 and Ser795 in MDA-MB-435 breast carcinoma cells with IC50 of 66 nM and 63 nM, respectively. PD 0332991 is a potent inhibitor of cell growth and suppresses DNA replication by preventing cells from entering S phase. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast (such as MDA-MB-435, MCF-7), colon (H1299), and lung carcinomas (Colo-205) as well as human leukemias (CRRF-CEM and K562), with IC50 values ranging from 0.04-0.17 μM. PD 0332991 significant increases the percentage of MDA-MB-453 in G1 period. [1] PD 0332991 inhibits phosphorylation of Rb in cycling CD138+ primary bone marrow myeloma cells, nontransformed primary B cells, MM1.S and CAG HMCLs cells line with IC50 of <0.1 μM, 0.05 μM, and 60-70 nM, respectively. PD 0332991 treatment also induces G1 arrest of CD138+ primary bone marrow myeloma and nontransformed primary B cells. PD 0332991 induces G1 arrest in MM1.S with IC50 of ~0.05 μM. [2] PD 0332991 preferentially inhibits proliferation of luminal estrogen receptor-positive (including HER2-positive) human breast cancer cell lines. PD 0332991 increases gene expression of pRb and cyclin D1 and decreases gene expression of CDKN2A (p16) in most sensitive lines. PD 0332991 enhances sensitivity to tamoxifen in cell lines with conditioned resistance to ER blockade. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H157 NF3nfIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mny3NE0yODBizszN MlPaO|IhcA>? NFv1PGFKSzVyPUmg{txO NILZUXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NFM1Oid-Mk[zPVA{PDJ:L3G+
H2170 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUezV|BLOC1zMECg{txO M2\JUlczKGh? NFHT[mFKSzVyPUWg{txO MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7MEO0Nkc,OjZ|OUCzOFI9N2F-
H520 NWDmZY9vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIq3cGgxNTFyMDFOwG0> NF3VV3c4OiCq MkPOTWM2OD1yLkezJO69VQ>? MmDoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUCzOFIoRjJ4M{mwN|QzRC:jPh?=
H596 M3HNRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDUbIllOC1zMECg{txO MY[3NkBp MWfJR|UxRTF{IN88US=> NHrubJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NFM1Oid-Mk[zPVA{PDJ:L3G+
IMR-32 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUS0POKhcA>? Mk\NSG1UVw>? MmDXTWM2OD1{NkGgcm0> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ{NUGyN{c,OjZ{MkWxNlM9N2F-
SH-SY5Y NGXrVJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi5NY81QMLiaB?= NFji[IVFVVOR MXvJR|UxRTZ5NjDuUS=> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ{NUGyN{c,OjZ{MkWxNlM9N2F-
NGP NW\PXXpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[5OFjDqGh? MYrEUXNQ MkHITWM2OD1{LkC3O{DPxE1? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ{NUGyN{c,OjZ{MkWxNlM9N2F-
SH-EP Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVixW406PDkEoHi= NHLGO3FFVVOR MUfJR|UxRTJwMkGxJO69VQ>? MlrOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{MkWxNlMoRjJ4MkK1NVI{RC:jPh?=
IMR-32 NIj4b|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TRRlEh|ryP M4ntWlI1KGh? MoHFSG1UVw>? NUfKUYxucW6mdXPld{BIOSCjcoLld5Q> M1fHTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkK1NVI{Lz5{NkKyOVEzOzxxYU6=
SH-SY5Y MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rYXlEh|ryP MXmyOEBp MoCySG1UVw>? NVXIfGg{cW6mdXPld{BIOSCjcoLld5Q> M1zCZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkK1NVI{Lz5{NkKyOVEzOzxxYU6=
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SH-EP NXrmb|BlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxJO69VQ>? MkfRNlQhcA>? M1\iTGROW09? NGHXUpVqdmS3Y3XzJGcyKGG{cnXzeC=> M4DkeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkK1NVI{Lz5{NkKyOVEzOzxxYU6=
NGP M1XmcmZ2[3Srb36gRZN{[Xl? M4fyfVAuOSEQvF2= MkDnNlQhcA>? NXP2bo9NTE2VTx?= MoHIdoVlfWOnczD0bIUh\XiycnXzd4lwdiCxZtMgWG9ROkFuwrDDR25GOixiYX7kxsBVUzIEoHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MnK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{MkWxNlMoRjJ4MkK1NVI{RC:jPh?=
IMR-32 NV36SlQ5TnWldHnvckBCe3OjeR?= M3f2N|AuOSEQvF2= NITMe|UzPCCq NYj2ZlVPTE2VTx?= MWTy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKG:owrDUU3AzSS{EoFPDUmUzNCCjbnVCpHRMOcLiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2PvPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkK1NVI{Lz5{NkKyOVEzOzxxYU6=
U-CH2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHoU|MxNTFizszN NVXVd5JzPzJiaB?= M1XUR2lEPTB;NUCuNkBvVQ>? NYLIVZZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFM6OjVpPkK2NVg{QTJ3PD;hQi=>
U-CH3 NWrpd2E3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\NNE0yKM7:TR?= M1S4SVczKGh? MlPLTWM2OD13MjDuUS=> Ml\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOEO5NlUoRjJ4MUizPVI2RC:jPh?=
U-CH6 M3PxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn25NE0yKM7:TR?= NGD0UHg4OiCq NFG0bYhKSzVyPUmwJI5O M1LNflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUizPVI2Lz5{NkG4N|kzPTxxYU6=
U-CH7 NEXCUlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\afVAuOSEQvF2= NISzPIU4OiCq MmPaTWM2OD17ODDuUS=> NYfVemllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFM6OjVpPkK2NVg{QTJ3PD;hQi=>
U-CH11 NYTpd2N{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mme5NE0yKM7:TR?= M4rBNFczKGh? M3XKZmlEPTB;M{SwJI5O NX33N5B7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFM6OjVpPkK2NVg{QTJ3PD;hQi=>
MCF7 NHPjWpFHfWO2aX;uJGF{e2G7 NY\sR29GOi53LUK1NEBvVQ>? NITHN|IzPCCq MoLYdoVlfWOnczDSZkBxcG:|cHjvdplt[XSrb36= NEPGflk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm5NVgyPyd-MkW5PVE5OTd:L3G+
MV4-11 Mn3BRZBweHSxc3nzJGF{e2G7 NHuzRooxNjVizszN MV:yOEBp MojU[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWlZXSgZpkhe2:{YX\lcoljKGGwZDDBR|IzOA>? NX;nWGh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFc6OTdpPkK1OFg4QTF5PD;hQi=>
MOLM13 NF;sR5RCeG:ydH;zbZMhSXO|YYm= NV\zZmJoOC53IN88US=> NVuxOJNHOjRiaB?= NUPkU2tJ\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXj[YQh[nlic3;yZYZmdmmkIHHu[EBCSzJ{MB?= NEnDb|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4O|kyPyd-MkW0PFc6OTd:L3G+
MOLM13-ITD alone NHLRN49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTvVpM{UUN3ME2wMlA5QSEEsTCwMlAxQSEQvF2= NX:ybFdZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFc6OTdpPkK1OFg4QTF5PD;hQi=>
MV4-11-ITD alone NF3qcplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXu2[ZdKUUN3ME2wMlA6OiEEsTCwMlAxQCEQvF2= M{\ORlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEi3PVE4Lz5{NUS4O|kyPzxxYU6=
MOLM13-ITD/D835Y MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnG5TWM2OD1yLkGxOEDDuSByLkCxNUDPxE1? M4\yUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEi3PVE4Lz5{NUS4O|kyPzxxYU6=
MV4-11-ITD/D835V NYDFXJpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGS3eYdKSzVyPUCuNVE3KMLzIECuNFEyKM7:TR?= NUnEN|R7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFc6OTdpPkK1OFg4QTF5PD;hQi=>
MV4-11-ITD/D835V M2P2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHv[oJKSzVyPUCuNVAzKMLzIECuNFA3KM7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR6N{mxO{c,OjV2OEe5NVc9N2F-
MV4-11-ITD/F691L MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moj4TWM2OD1yLkGxNkDDuSByLkCxOUDPxE1? NXLqfWtQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFc6OTdpPkK1OFg4QTF5PD;hQi=>
MV4-11-ITD/N841K MkTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXRV|dvUUN3ME2wMlEyOyEEsTCwMlAxOiEQvF2= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR6N{mxO{c,OjV2OEe5NVc9N2F-
U937-FLT3 WT NWXadlBuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWeydW5XUUN3ME2wMlExOiEEsTCwMlAyOyEQvF2= M1\Md|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEi3PVE4Lz5{NUS4O|kyPzxxYU6=
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697 NHvyZohIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MXzJR|UxKD1iMD6xOFg{QCEQvF2= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NB69 M3vydWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 M{S2Z2lEPTBiPTCwMlE3OThizszN NVr1ZmM1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
EoL-1-cell NF\IUZBIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MWTJR|UxKD1iMD6xPFczPiEQvF2= M4XmR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
BHT-101 Ml2wS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? NFG4RXhKSzVyIE2gNE4yQTh{NTFOwG0> NHXMeIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
SK-NEP-1 M2jENWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 MUfJR|UxKD1iMD6yNlAxOiEQvF2= NFfJcGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
MHH-NB-11 NYm3UnpVT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MnTZTWM2OCB;IECuNlIxOTlizszN M4LPUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
AsPC-1 NHvrZnpIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MWXJR|UxKD1iMD6yOVI2OyEQvF2= MmjqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
ES1 M37UUmdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 Ml7KTWM2OCB;IECuNlU3OjVizszN MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
LAMA-84 MkTKS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? M4n0e2lEPTBiPTCwMlI2QDF7IN88US=> MlnNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
MOLT-16 NHqweGpIem:5dHigTY5pcWKrdHnvckBie3OjeR?= M2HhVGlEPTBiPTCwMlI2QDR7IN88US=> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
ES7 MUDHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? MnWyTWM2OCB;IECuNlc{ODlizszN NV:4dWhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
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J-RT3-T3-5 NEX6eHRIem:5dHigTY5pcWKrdHnvckBie3OjeR?= M2HEXWlEPTBiPTCwMlk{PjB4IN88US=> M3u4UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
Mewo NGLHSI9Iem:5dHigTY5pcWKrdHnvckBie3OjeR?= NXLNPHVbUUN3MDC9JFAvQTN4NjFOwG0> NF[wTYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
NCI-H1770 M2fyOWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 Mn\tTWM2OCB;IECuPVQxPTVizszN NF[0ZWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
HO-1-N-1 M{DXPGdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 M1HkW2lEPTBiPTCwMlk3OjhzIN88US=> MlzzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
HSC-3 NVLj[GFKT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MWXJR|UxKD1iMD65OlY1QCEQvF2= NVPacI5sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
TYK-nu NVyyU2I5T3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= M13tZmlEPTBiPTCwMlk6QDJ3IN88US=> NHjwVoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
KYSE-150 NGLuOGFIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MoTLTWM2OCB;IEGuNFAxPzZizszN M{XieFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
SN12C MlfyS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? MkPrTWM2OCB;IEGuNFA5PzVizszN NXr5UGNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
MOLT-13 MVXHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? NVzFe4dLUUN3MDC9JFEvODF2MkGg{txO MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
TE-11 NXfnc5pbT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MkLQTWM2OCB;IEGuNFQ5OTJizszN NYfZS|FiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
DB MWHHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? NHvGU21KSzVyIE2gNU4xPzJ5MzFOwG0> NYfZSI5wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
CAL-39 NF;6T5pIem:5dHigTY5pcWKrdHnvckBie3OjeR?= M4WybWlEPTBiPTCxMlA4PTJ{IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
A3-KAW Mlr5S5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? NHz0fndKSzVyIE2gNU4xQDRyODFOwG0> MkjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
CHP-134 M1HkOGdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 M2jTTmlEPTBiPTCxMlEyQDB5IN88US=> M3zO[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
TGW NUjjTFh6T3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MoX5TWM2OCB;IEGuNVI{QTVizszN MmHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
QIMR-WIL M1uwdGdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 NHX4eohKSzVyIE2gNU4yOzF|NDFOwG0> NVjuZnFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
NCI-SNU-1 NX7qcpRyT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MXPJR|UxKD1iMT6xOlM2PCEQvF2= NXzm[INKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
CGTH-W-1 MXjHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? MomwTWM2OCB;IEGuNVcyQDZizszN M4XXfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
MHH-ES-1 NE\SXJhIem:5dHigTY5pcWKrdHnvckBie3OjeR?= NHHCVI5KSzVyIE2gNU4yPzl6NjFOwG0> MlHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
LB2241-RCC NHrNVVVIem:5dHigTY5pcWKrdHnvckBie3OjeR?= NGHKOppKSzVyIE2gNU4yQDZ{IN88US=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
ML-2 MlPjS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? NHPqfXVKSzVyIE2gNU4zODd|NDFOwG0> Ml3OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
COR-L23 M2[1UGdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 NX:0eZBuUUN3MDC9JFEvOjJ7M{Og{txO NIm5NIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
BFTC-905 NIrCR5ZIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MmfETWM2OCB;IEGuNlQzPjdizszN NV7BUYZkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
Hs-578-T MX3Hdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? MkDQTWM2OCB;IEGuNlU5OTdizszN NXLSbpNlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
KG-1 M3SydWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 NX7RbHBOUUN3MDC9JFEvOjZ4OE[g{txO NEn1VZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
HEL M4DWR2dzd3e2aDDJcohq[mm2aX;uJIF{e2G7 NY\rfWVsUUN3MDC9JFEvOjl|M{ig{txO NUPVPGVURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
A549 MmfaS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? NWrXNYlMUUN3MDC9JFEvOjl|OUmg{txO MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
COLO-741 MmOyS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? M2DPVWlEPTBiPTCxMlMzODh7IN88US=> Mmi0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
PC-3 M2XxdWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 NFHaboVKSzVyIE2gNU4{PTJ{MTFOwG0> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
HOS MYXHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? Mo\wTWM2OCB;IEGuN|UzQTZizszN MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
HT-1080 M3fVTGdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 M1m1SGlEPTBiPTCxMlM4PTF7IN88US=> M3LXb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
TE-8 NGrwXmFIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MYHJR|UxKD1iMT60NVc4PCEQvF2= NUH4Tm8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
BHY NV3p[lV1T3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MmHOTWM2OCB;IEGuOFY6OjNizszN NYHkOGt[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
BB65-RCC NHruRYpIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MXTJR|UxKD1iMT61NFUzQCEQvF2= MonGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
HN M3HB[mdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 M3TNN2lEPTBiPTCxMlU1ODdzIN88US=> M{n6NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
NCI-H441 M3XUbWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 MWLJR|UxKD1iMT61OFkxPyEQvF2= M3e4NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
RPMI-8866 MX;Hdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? NU\mXWs2UUN3MDC9JFEvPTh3MEeg{txO NG[yUZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
CAL-62 MVzHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? MmTWTWM2OCB;IEGuOlA5PjJizszN Mm\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
MG-63 MnKxS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? MlTLTWM2OCB;IEGuOlE5OTNizszN MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
SK-LU-1 NEnyd4tIem:5dHigTY5pcWKrdHnvckBie3OjeR?= NXvHW3U2UUN3MDC9JFEvPjJzNUKg{txO NIjCem09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
BCPAP MoXIS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? M2rOXmlEPTBiPTCxMlY3PDV5IN88US=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
22RV1 Mo\IS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? MlfDTWM2OCB;IEGuOlc5PDNizszN NVLp[GtHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
T47D NGjXVVRIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MmT4TWM2OCB;IEGuOlgxPjFizszN M2[wb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
MSTO-211H NUDtW4NET3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= M{fWOmlEPTBiPTCxMlY6PjB|IN88US=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
DEL MVPHdo94fGhiSX7obYJqfGmxbjDhd5NigQ>? MmDSTWM2OCB;IEGuO|AzPzNizszN NF;WSpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
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LAN-5 NUX5Wm1GeUiWUzDhd5NigQ>? NW\FSlVKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 MUHxTHRUKGG|c3H5 NWfSdowyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= MlLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
RB1 (pT821) / RB1 (pS780); 

PubMed: 30300583     


Immunoblots showing dose-dependent impact of 72 hr palbociclib treatment on indicated protein levels in Kasumi-1 and SKNO-1 cells.

pAMPKα(T172) / AMPKα; 

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. 

pULK1(S317) / ULK1; 

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. 

c-Jun / p-c-Jun / NFκB(p50); 

PubMed: 26540629     


The expression of c-Jun and phosphorylated c-Jun was assessed using western blot after the cells were treated with palbociclib. 

p38 / p-P38 / JNK / p-JNK; 

PubMed: 26540629     


MAPK pathway-related proteins, p38, ERK, JNK expression levels were detected.

30300583 28453226 26540629
Growth inhibition assay
Cell viability; 

PubMed: 28453226     


Dose- and time-dependent effects of palbociclib on cell viability in three HCC cell lines. Hep3B, Huh7, and PLC5 cells were treated with palbociclib at the indicated concentrations for 24 or 48 h and assayed by MTT. The solvent (DMSO) concentration in each sample is equal (0.7%).

IC50; 

PubMed: 27099147     


Dose-response curve of ITD+ (red) or control (black) leukemic cells with CDK4/6 inhibitor palbociclib. Cells were incubated with increasing concentrations for 72 hours. Cell viability and proliferation were assessed by using the CTG assay. IC50 values were calculated by using GraphPad Prism software. Error bars indicate ± SEM.

28453226 27099147
Immunofluorescence
γH2AX(Ser139); 

PubMed: 29669860     


Representative maximum‐intensity projections of MCF7 cells treated with the 1 μM palbociclib and/or 7.5 nM bortezomib. Note that 7.5 nM bortezomib inhibits proteasome only partially. Fixed and permeabilized cells were stained with Alexa Fluor 488‐conjugated Ki67 antibody, Alexa Fluor 647‐conjugated phospho‐Histone H2A.X (γH2AX) (pSer139) antibody, and DAPI. All images were acquired with the same magnification, and scale bar is 20 μm.

LC3B; 

PubMed: 28453226     


LC3B immunofluorescence in palbociclib‐treated Hep3B cells. Arrowheads indicate LC3‐positive autophagosomes. Nuclei were counterstained with DAPI (blue). 

29669860 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(150 mg/kg) produces rapid Colo-205 colon carcinoma xenografts regressions and a corresponding tumor growth delay. PD 0332991 (150 mg/kg) induces complete tumor stasis and cell kill in MDA-MB-435 breast carcinoma. PD 0332991 (150 mg/kg) also induces significant tumor regression in mice bearing the SF-295 glioblastoma xenografts, and in ZR-75-1 breast and PC-3 prostate tumor models (complete suppression of tumor growth). PD 0332991 (150 mg/kg) suppresses Rb Ser780 phosphorylation in MDA-MB-435 breast carcinoma over the full 24-hour period. PD 0332991 (150 mg/kg) down-regulates expression of four E2F-regulated genes CDC2, CCNE2, TK1, and TOP2A in Colo-205 carcinoma xenografts. [1] PD 0332991 also rapidly inhibits myeloma tumor growth. [2]

Protocol

Kinase Assay:[4]
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CDK activity assays:

CDK assays for IC50 determinations and kinetic evaluation 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 reaction volume 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) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST•RB-Cterm, and appropriate dilutions of inhibitor. All components except the [γ-32P]ATP are added to the wells, and placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP, and incubated at 25℃ for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid, and the plate is kept at 4 ℃ for at least 1 hr to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% trichloroacetic acid, and radioactive incorporation is determined with a β plate counter.
Cell Research:[3]
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  • Cell lines: Human breast cancer cells MDA-MB-435
  • Concentrations: 2 μM
  • Incubation Time: 6 days
  • Method: Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of PD 0332991 are added. Control wells without drug are also seeded. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter Z2 particle counter.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Human colon carcinoma xenografts Colo-205
  • Dosages: 150 mg/kg
  • Administration: o.p. injection every day
    (Only for Reference)

Solubility (25°C)

In vitro Water 10 mg/mL warmed (17.43 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
saline (with warming)
For best results, use promptly after mixing.
10mg/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 573.66
Formula

C24H29N7O2.C2H6O4S

CAS No. 827022-33-3
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.C(CS(=O)(=O)O)O

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
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.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    What is the best vehicle for palbociclib for in vitro and in vivo?

  • Answer:

    You can use water for vitro use and Saline for vivo use.

CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID