Palbociclib (PD0332991) Isethionate

Licensed and Manufactured by Pfizer Catalog No.S1579

For research use only.

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.

Palbociclib (PD0332991) Isethionate Chemical Structure

CAS No. 827022-33-3

Selleck's Palbociclib (PD0332991) Isethionate has been cited by 253 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 NF3JfoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHONE0yODBizszN NUP6eGt2PzJiaB?= M4HCZWlEPTB;OTFOwG0> NFjxcGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5NFM1Oid-Mk[zPVA{PDJ:L3G+
H2170 MnvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPtNE0yODBizszN MVy3NkBp MmS5TWM2OD13IN88US=> NUDKSoR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVA{PDJpPkK2N|kxOzR{PD;hQi=>
H520 NX\ZfnVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz2bpcxNTFyMDFOwG0> MXe3NkBp NW[1SYZJUUN3ME2wMlc{KM7:TR?= NVzKV3hyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVA{PDJpPkK2N|kxOzR{PD;hQi=>
H596 M3;OPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XzXFAuOTByIN88US=> NF[5e4k4OiCq NXH4U3g{UUN3ME2xNkDPxE1? MlXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUCzOFIoRjJ4M{mwN|QzRC:jPh?=
IMR-32 MoHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTSdGQ1QMLiaB?= MoHvSG1UVw>? NEnhUpFKSzVyPUK2NUBvVQ>? NW[xcVk2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNlUyOjNpPkK2NlI2OTJ|PD;hQi=>
SH-SY5Y NFy5SlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULQ[pBrPDkEoHi= NFjt[ZdFVVOR NFv5OWdKSzVyPU[3OkBvVQ>? NVP2VJJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNlUyOjNpPkK2NlI2OTJ|PD;hQi=>
NGP NF72S5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DRZ|Q5yqCq MmnESG1UVw>? NWXyXHl2UUN3ME2yMlA4PyEQvF2= NV;rd|BbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNlUyOjNpPkK2NlI2OTJ|PD;hQi=>
SH-EP NIjPdldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjjeoc1QMLiaB?= NX7FUnNETE2VTx?= MmK4TWM2OD1{LkKxNUDPxE1? M{TZOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkK1NVI{Lz5{NkKyOVEzOzxxYU6=
IMR-32 NVP0[WR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH3T4cyKM7:TR?= NHLCW4UzPCCq NYqzWIU3TE2VTx?= Mn\YbY5lfWOnczDHNUBienKnc4S= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ{NUGyN{c,OjZ{MkWxNlM9N2F-
SH-SY5Y MmHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T3bVEh|ryP MUGyOEBp M4jZcWROW09? MUDpcoR2[2W|IFexJIFzemW|dB?= MoriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{MkWxNlMoRjJ4MkK1NVI{RC:jPh?=
NGP M4DWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPSNUDPxE1? NWqzeWJLOjRiaB?= NUPGU2wyTE2VTx?= NV70eXNicW6mdXPld{BIOSCjcoLld5Q> NVPaXVF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yNlUyOjNpPkK2NlI2OTJ|PD;hQi=>
SH-EP NGLtVYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\STVEh|ryP MWOyOEBp NHXPfndFVVOR NEG2XFBqdmS3Y3XzJGcyKGG{cnXzeC=> NGXn[oE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKyOVEzOyd-Mk[yNlUyOjN:L3G+
NGP M1WyUGZ2[3Srb36gRZN{[Xl? NIXmSooxNTFizszN MWiyOEBp MUHEUXNQ M3P5fJJm\HWlZYOgeIhmKGW6cILld5Nqd25ib3dCpHRQWDKDLNMgR2NPTTJuIHHu[OKhXEtzwrDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ{NUGyN{c,OjZ{MkWxNlM9N2F-
IMR-32 M3PwVGZ2[3Srb36gRZN{[Xl? NX;xWGdiOC1zIN88US=> MXeyOEBp M4roUmROW09? NXrPNItJemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[uKhXE:SMlGsxsBES06HMjygZY5lyqCWS{JCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2Cwe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MkK1NVI{Lz5{NkKyOVEzOzxxYU6=
U-CH2 M13DT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLHNE0yKM7:TR?= MmnyO|IhcA>? NXXBZYR2UUN3ME21NE4zKG6P NXXsR5VCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFM6OjVpPkK2NVg{QTJ3PD;hQi=>
U-CH3 NFL2PFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\sR3ZtOC1zIN88US=> NUDRR4hqPzJiaB?= M2rkTGlEPTB;NUKgcm0> M3HiT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUizPVI2Lz5{NkG4N|kzPTxxYU6=
U-CH6 M3P6Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1KwPVAuOSEQvF2= NH[1cGI4OiCq M2K2WWlEPTB;OUCgcm0> MmPjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOEO5NlUoRjJ4MUizPVI2RC:jPh?=
U-CH7 M1zhZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlToNE0yKM7:TR?= NHTROmc4OiCq NGXFXXRKSzVyPUm4JI5O M3\rUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUizPVI2Lz5{NkG4N|kzPTxxYU6=
U-CH11 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmwMVEh|ryP NVvwbJRTPzJiaB?= MUfJR|UxRTN2MDDuUS=> NWXLdHRrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFM6OjVpPkK2NVg{QTJ3PD;hQi=>
MCF7 MlTUSpVkfGmxbjDBd5NigQ>? NWHIOpJyOi53LUK1NEBvVQ>? NH;xNmkzPCCq NEHMSYxz\WS3Y3XzJHJjKHCqb4PwbI9zgWyjdHnvci=> NVm5cWlmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5PVE5OTdpPkK1PVkyQDF5PD;hQi=>
MV4-11 NXq0b5VPSXCxcITvd4l{KEG|c3H5 Mn3vNE42KM7:TR?= MVyyOEBp M3L6V4VvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KHOxcnHm[Y5q[iCjbnSgRWMzOjB? NEPSNVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4O|kyPyd-MkW0PFc6OTd:L3G+
MOLM13 NEi1Zo1CeG:ydH;zbZMhSXO|YYm= NUHwc|lXOC53IN88US=> NUHLcXNHOjRiaB?= NITLWW1mdmijbnPld{BieG:ydH;zbZMhcW6mdXPl[EBjgSC|b4Lh[oVvcWJiYX7kJGFEOjJy MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR6N{mxO{c,OjV2OEe5NVc9N2F-
MOLM13-ITD alone Mnq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXsfnRKSzVyPUCuNFg6KMLzIECuNFA6KM7:TR?= MmXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2OEe5NVcoRjJ3NEi3PVE4RC:jPh?=
MV4-11-ITD alone NH63NW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUiyXolvUUN3ME2wMlA6OiEEsTCwMlAxQCEQvF2= NIW2dVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4O|kyPyd-MkW0PFc6OTd:L3G+
MOLM13-ITD/D835Y MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfCUZVKSzVyPUCuNVE1KMLzIECuNFEyKM7:TR?= NX;WPVZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFc6OTdpPkK1OFg4QTF5PD;hQi=>
MV4-11-ITD/D835V NV;iXWFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwMUG2JOKyKDBwMEGxJO69VQ>? M4W1clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEi3PVE4Lz5{NUS4O|kyPzxxYU6=
MV4-11-ITD/D835V MmXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljQTWM2OD1yLkGwNkDDuSByLkCwOkDPxE1? NX:zdGV{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW0PFc6OTdpPkK1OFg4QTF5PD;hQi=>
MV4-11-ITD/F691L NUj1S2JST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDhWHVVUUN3ME2wMlEyOiEEsTCwMlAyPSEQvF2= NFzN[os9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4O|kyPyd-MkW0PFc6OTd:L3G+
MV4-11-ITD/N841K M3\lU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfzbYg5UUN3ME2wMlEyOyEEsTCwMlAxOiEQvF2= NHrQeYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUS4O|kyPyd-MkW0PFc6OTd:L3G+
U937-FLT3 WT MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHYTWM2OD1yLkGwNkDDuSByLkCxN{DPxE1? MlzRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2OEe5NVcoRjJ3NEi3PVE4RC:jPh?=
P12-ICHIKAWA NGTPZnBIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MkXHTWM2OCB;IECuNFk3ODRizszN MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
697 MlPtS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? MYfJR|UxKD1iMD6xOFg{QCEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
NB69 NEC3dY9Iem:5dHigTY5pcWKrdHnvckBie3OjeR?= NWDHRlNVUUN3MDC9JFAvOTZzODFOwG0> NUjTSYp[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
EoL-1-cell NWrGTGFXT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= NGrDbYtKSzVyIE2gNE4yQDd{NjFOwG0> M1jUUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
BHT-101 NXvxfXA{T3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MlPITWM2OCB;IECuNVk5OjVizszN MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
SK-NEP-1 NYnqZ4lsT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= NX:2Z3JnUUN3MDC9JFAvOjJyMEKg{txO NX;RZpJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
MHH-NB-11 Mn2xS5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? Mme5TWM2OCB;IECuNlIxOTlizszN MnPtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
AsPC-1 M37lXWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 MnjGTWM2OCB;IECuNlUzPTNizszN NYq4XYVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTh7OU[zM{c,W0GQR1XSQE9iRg>?
ES1 NHz6d3RIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MVHJR|UxKD1iMD6yOVYzPSEQvF2= M4rsWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
LAMA-84 NUC4WYVNT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MlvDTWM2OCB;IECuNlU5OTlizszN NIjR[VA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
MOLT-16 M2q0[mdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 MUnJR|UxKD1iMD6yOVg1QSEQvF2= NFGxdWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
ES7 M1HXPWdzd3e2aDDJcohq[mm2aX;uJIF{e2G7 NYfVd4FkUUN3MDC9JFAvOjd|MEmg{txO MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
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COR-L23 NE[0fYlIem:5dHigTY5pcWKrdHnvckBie3OjeR?= M13vSWlEPTBiPTCxMlIzQTN|IN88US=> NGruOmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
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BB65-RCC NIHPZo9Iem:5dHigTY5pcWKrdHnvckBie3OjeR?= MVzJR|UxKD1iMT61NFUzQCEQvF2= M2XwV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
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RPMI-8866 Mn24S5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? NF3wdJNKSzVyIE2gNU42QDVyNzFOwG0> M{WxS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5QTl4Mz:nQnNCVkeHUkyvZV4>
CAL-62 NFTheWxIem:5dHigTY5pcWKrdHnvckBie3OjeR?= M{jtTGlEPTBiPTCxMlYxQDZ{IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
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22RV1 MkT3S5Jwf3SqIFnubIljcXSrb36gZZN{[Xl? MYLJR|UxKD1iMT62O|g1OyEQvF2= MmLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVg6QTZ|Lze+V2FPT0WUPD;hQi=>
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DEL NULyW5FCT3Kxd4ToJGlvcGmkaYTpc44h[XO|YYm= MUHJR|UxKD1iMT63NFI4OyEQvF2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPFk6PjNxJ{7TRW5ITVJ:L3G+
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JEG-3 NEP6OotIem:5dHigTY5pcWKrdHnvckBie3OjeR?= MnHNTWM2OCB;IES0Mlk1PyEQvF2= NEDaW5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDl7NkOvK|5USU6JRWK8M4E,
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Rh18 MUPxTHRUKGG|c3H5 MoG1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NUDVWWZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot RB1 (pT821) / RB1 (pS780) ; pAMPKα(T172) / AMPKα ; pULK1(S317) / ULK1 ; c-Jun / p-c-Jun / NFκB(p50) ; p38 / p-P38 / JNK / p-JNK 30300583 28453226 26540629
Growth inhibition assay Cell viability ; IC50 28453226 27099147
Immunofluorescence γH2AX(Ser139) ; LC3B 29669860 28453226
ELISA PGE2 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 (from reference)

Kinase Assay:[4]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: Human colon carcinoma xenografts Colo-205
  • Dosages: 150 mg/kg
  • Administration: o.p. injection every day

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 (with warming)
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 573.66
Formula

C24H29N7O2.C2H6O4S

CAS No. 827022-33-3
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.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)

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

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

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