Palbociclib (PD0332991) Isethionate

Pfizer辉瑞授权生产 目录号:S1579

Palbociclib (PD0332991) Isethionate Chemical Structure

Molecular Weight(MW): 573.66

Palbociclib (PD0332991) Isethionate是一种高度选择性的CDK4/6抑制剂,无细胞试验中IC50为11 nM/16 nM,对CDK1/2/5,EGFR,FGFR,PDGFR, InsR等没有抑制活性。Phase 3。

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RMB 3026.06 现货
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客户使用该产品的9个实验数据:

  • (C) In vivo treatment of Tg:Pomc-Pttg;Pomc-eGFP embryos with small-molecule CDK inhibitors (50μM) or 0.2% DMSO as control from 18 to 40 hpf. One hundred to one hundred fifty embryos were treated with each compound. Representative images of live embryos are shown with gross morphology (Right) and pituitary Pomc-GFP–positive cells at higher magnification (Left) at 40 hpf. Embryos exposed to flavopiridol developed early developmental defect before pituitary POMC cell ontogeny occurs. (D) Relative expression of pituitary Pomc-eGFP fluorescence analyzed using Volocity 5.2 software (Improvision; mean ±SE of relative expression, n = 7). (E) R-roscovitine specifically suppresses expansion of pituitary POMC cells overexpressing zPttg from 18 to 48 hpf. Double transgenic Tg:Pomc-Pttg;Prl-RFP embryos were generated by breeding Tg:Pomc-Pttg fish with a previously generated PRL-RFP transgenic line, in which RFP was targeted to pituitary lactotrophs by a zebrafish Prolactin promoter (34). Representative fluorescent microscopy of pituitary POMC-eGFP (a and b) and PRL-RFP (c and d) expression in live Tg:Pomc-Pttg; Pomc-eGFP and Tg:Pomc-Pttg;Prl-RFP embryos treated with 0.2% DMSO (a and c) or 50 μM R-roscovitine (b and d). (F) Relative expression of pituitary POMC-eGFP or PRL-RFP fluorescence were analyzed (mean ±SE of relative expression; n = 10). Results represent one of three similar experiments;*P < 0.02 and **P < 0.000005. (Scale bar, 50 μm.)

    PNAS 2011 108(20), 8414-9. Palbociclib (PD0332991) Isethionate purchased from Selleck.

    Potentiation of SFN-induced cytotoxicity by a panel of CDK inhibitors in MDA-MB-231 cells. The fraction of cells killed (Fa ±SEM) by SFN in the presence of DMSO (vehicle) or a fixed concentration (0.2 uM) of PD0332991. The fraction of cells killed by CDK inhibitors at a fixed concentration of 0.2 uM is shown for comparison [dashed lines; gray shading (±SEM)]. MDE-CI analysis of drug interactions in the upper panels. CIs as a function of SFN concentration are shown. Black, gray, and white bars denote synergistic (CI < 0.9), additive (CI = 0.9-1.1), or antagonistic interactions (CI > 1.1), respectively. Synergistic ratios and SFN-EC50 are indicated. Data are representative of two to three independent experiments.

    Neoplasia 2013 15(8), 939-51. Palbociclib (PD0332991) Isethionate purchased from Selleck.

  • HT29 cells were treated with DMSO control, 1 uM selumetinib (Sel) or 5 uM PD0332991 (991) for 24 or 48 h after which time cells were lysed, subjected to SDS/PAGE and immunoblotted with the indicated antibodies.

    Biochem J 2014 459(3), 513-24. Palbociclib (PD0332991) Isethionate purchased from Selleck.

     

    Patient tumor cell sensitivity to combinatorial treatment with histone deacetylase (HDAC)/cyclin-dependent kinase (CDK) inhibitors in 3-D culture. The effect of each drug or drug combination was assessed by fluorescent dye to identify live (green) and dead cells (red). Cells from breast reduction patients were used as non-cancer control in the assay.

    Pharmacogenomics J 2013 13(1), 94-104. Palbociclib (PD0332991) Isethionate purchased from Selleck.

  • Immunoblot analysis of PD0332991-induced senescence in MEL10 cells. Cells were treated with indicated concentrations of PD0332991 with or without 10 nM rapamycin. After 1 day, cells were lysed and immunoblotting was performed with the indicated antibodies.

    Cell Cycle 2013 12(18), 3063-9. Palbociclib (PD0332991) Isethionate purchased from Selleck.

    Int J Mol Med, 2018, 41(5):2473-2484. Palbociclib (PD0332991) Isethionate purchased from Selleck.

  • Western blot analysis shows inhibition of Rb phosphorylation at the protein level, with inhibition of PD-0332991 observed at 2uM in the PDGF-B; Ink4a-ARF deficient line after only 24 hours of treatment.

    PLoS One 2013 8(10), e77639. Palbociclib (PD0332991) Isethionate purchased from Selleck.

     

    Cdk4 is upregulated in ARMS and mMSCs transfected with PAX7-FKHR fusion gene (MP7F), and can be specifi cally inhibited. D: IF results showing overexpression of cdk4 in MP7F cells compared to parental mMSCs and reduced expression of cdk4 after treatment of MP7F cells with the cdk4 inhibitor, PD-0332991. E: IF results showing MyoD1 expression in parental mMSCs cells, and MP7F cells untreated and after treatment with the cdk4 inhibitor, PD-0332991.

    Clin Transl Oncol 2012 14(3), 197-206 . Palbociclib (PD0332991) Isethionate purchased from Selleck.

  • Different breast cancer cell lines were seeded in 96 well plates and treated with different concentrations of PD0332991. After 72h, cell viability was assessed by MTT. Data shows that these cancer cell lines had a better response to CDK4/6 inhibition than the less tumorigenic MCF10A-Ras cells.

    Helen Sadik from Johhns Hopkins University. Palbociclib (PD0332991) Isethionate purchased from Selleck.

产品安全说明书

CDK抑制剂选择性比较

生物活性

产品描述 Palbociclib (PD0332991) Isethionate是一种高度选择性的CDK4/6抑制剂,无细胞试验中IC50为11 nM/16 nM,对CDK1/2/5,EGFR,FGFR,PDGFR, InsR等没有抑制活性。Phase 3。
特性 PD 0332991治疗多种癌症,特异性抑制CDK4/6,是第一种有前途的抑制剂。
靶点
CDK4/CyclinD3 [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
CDK6/CyclinD2 [1]
(Cell-free assay)
9 nM 11 nM 15 nM
体外研究

PD 0332991对CDK4/6具有绝对选择性,对其他CDKs几乎没有抑制活性。PD 0332991作用于MDA-MB-435乳腺癌细胞,有效降低Rb在Ser780 和 Ser795位点磷酸化,IC50分别为66 nM和63 nM。PD 0332991通过抑制细胞进入S期,有效抑制细胞生长,抑制 DNA复制。PD 0332991抑制胸苷渗透进Rb阳性人类乳腺癌(如MDA-MB-435, MCF-7), 结肠癌 (H1299), 和肺癌(Colo-205) 及白血病(CRRF-CEM和K562)的DNA中,IC50值为0.04-0.17 μM。PD 0332991显著增强MDA-MB-453在G1期的百分比。[1]PD 0332991作用于CD138+原发性骨髓瘤细胞,初级非转化的B细胞,MM1.S和CAG HMCLs细胞系,抑制Rb磷酸化,IC50分别为 <0.1 μM, 0.05 μM, 和 60-70 nM。PD 0332991作用于CD138+原发性骨髓瘤细胞和初级非转化的B细胞,诱导细胞停滞在G1期。PD 0332991诱导MM1.S细胞停滞在G1期,IC50为~0.05 μM。[2]PD 0332991优先抑制Luminal雌激素受体阳性(包括HER2阳性)人类乳腺癌细胞系。PD 0332991作用于大部分敏感的细胞系,促进pRb和cyclin D1基因表达,且降低CDKN2A(p16)基因表达。PD 0332991作用于条件性抗ER抑制的细胞系,增强对Tamoxifen的敏感性。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H157 M1\vZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLuZ3kxNTFyMDFOwG0> M3TyPVczKGh? NITzSGVKSzVyPUmg{txO MYeyOlM6ODN2Mh?=
H2170 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvmc5dwOC1zMECg{txO MUi3NkBp NH;BeVBKSzVyPUWg{txO NXj2d5RGOjZ|OUCzOFI>
H520 M1HmWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yzeVAuOTByIN88US=> MmL5O|IhcA>? NEL4W2tKSzVyPUCuO|Mh|ryP MkLXNlY{QTB|NEK=
H596 NVTUOoNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nI[VAuOTByIN88US=> MVO3NkBp NYLQSmtuUUN3ME2xNkDPxE1? Ml\XNlY{QTB|NEK=
IMR-32 MnraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzHOVM1QMLiaB?= NU\MdVFCTE2VTx?= MXHJR|UxRTJ4MTDuUS=> NYfaWJl{OjZ{MkWxNlM>
SH-SY5Y MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDofYs1QMLiaB?= M{HufmROW09? M{jpfWlEPTB;Nke2JI5O NUD0TmFkOjZ{MkWxNlM>
NGP MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPmeGdqPDkEoHi= NEDBVYRFVVOR NXjaOo1[UUN3ME2yMlA4PyEQvF2= MWKyOlIzPTF{Mx?=
SH-EP MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;2OFjDqGh? MWHEUXNQ NX7rfWtJUUN3ME2yMlIyOSEQvF2= MnvTNlYzOjVzMkO=
IMR-32 MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXFflQ5OSEQvF2= MUWyOEBp NIq5RnNFVVOR MVLpcoR2[2W|IFexJIFzemW|dB?= MXeyOlIzPTF{Mx?=
SH-SY5Y NH:3Uo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPWbpFYOSEQvF2= MnLSNlQhcA>? MnXoSG1UVw>? M1TlbIlv\HWlZYOgS|Eh[XK{ZYP0 NEPjd|IzPjJ{NUGyNy=>
NGP NFj1TYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXmxJO69VQ>? NFnkW5IzPCCq MVTEUXNQ MX7pcoR2[2W|IFexJIFzemW|dB?= MXeyOlIzPTF{Mx?=
SH-EP NHy5U3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP0Z2hKOSEQvF2= MmLMNlQhcA>? M{WyfmROW09? M1fxeYlv\HWlZYOgS|Eh[XK{ZYP0 M4nZPVI3OjJ3MUKz
NGP MYDGeYN1cW:wIFHzd4F6 MVmwMVEh|ryP MWqyOEBp MoL4SG1UVw>? NYPFO4ZuemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[uKhXE:SMlGsxsBES06HMjygZY5lyqCWS{JCpIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3fqUVI3OjJ3MUKz
IMR-32 NYrOeFlzTnWldHnvckBCe3OjeR?= MWGwMVEh|ryP MVKyOEBp NVXOTXl{TE2VTx?= NFHBToVz\WS3Y3XzJJRp\SCneIDy[ZN{cW:wIH;mxsBVV1B{QT|CpGNEVkV{LDDhcoTDqFSNMdMgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NVWyb41kOjZ{MkWxNlM>
U-CH2 NHKz[|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[yTFAuOSEQvF2= NX[1VFM1PzJiaB?= NY\nUIJ5UUN3ME21NE4zKG6P MXGyOlE5Ozl{NR?=
U-CH3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUiwMVEh|ryP NGHnPWk4OiCq NXTuTXZSUUN3ME21NkBvVQ>? MU[yOlE5Ozl{NR?=
U-CH6 NHnzWVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mof5NE0yKM7:TR?= NIW1T2I4OiCq MmSyTWM2OD17MDDuUS=> M4\jc|I3OTh|OUK1
U-CH7 M4LlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPp[mQxNTFizszN NYnMNJNjPzJiaB?= M{PKb2lEPTB;OUigcm0> MV:yOlE5Ozl{NR?=
U-CH11 NVmxRlNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknkNE0yKM7:TR?= NIjnTpI4OiCq M3T0XGlEPTB;M{SwJI5O NGXaXFAzPjF6M{myOS=>
MCF7 NIrGSFRHfWO2aX;uJGF{e2G7 MYKyMlUuOjVyIH7N NIjVT24zPCCq M4XHOZJm\HWlZYOgVoIheGixc4Doc5J6dGG2aX;u MWeyOVk6OThzNx?=
MV4-11 NYLR[INGSXCxcITvd4l{KEG|c3H5 M1fVR|AvPSEQvF2= MWCyOEBp NH21RXlmdmijbnPld{BieG:ydH;zbZMhcW6mdXPl[EBjgSC|b4Lh[oVvcWJiYX7kJGFEOjJy MkPwNlU1QDd7MUe=
MOLM13 M1mwUWFxd3C2b4Ppd{BCe3OjeR?= Mn7FNE42KM7:TR?= NXnMXYJ6OjRiaB?= NUPSd2NV\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXj[YQh[nlic3;yZYZmdmmkIHHu[EBCSzJ{MB?= MX6yOVQ5PzlzNx?=
MOLM13-ITD alone NVe5e3Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfxTWM2OD1yLkC4PUDDuSByLkCwPUDPxE1? MnLVNlU1QDd7MUe=
MV4-11-ITD alone MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHjTWM2OD1yLkC5NkDDuSByLkCwPEDPxE1? NICy[HUzPTR6N{mxOy=>
MOLM13-ITD/D835Y NV\RV3N2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMUG0JOKyKDBwMEGxJO69VQ>? NHzscFczPTR6N{mxOy=>
MV4-11-ITD/D835V MlvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMUG2JOKyKDBwMEGxJO69VQ>? MnvhNlU1QDd7MUe=
MV4-11-ITD/D835V MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DCRWlEPTB;MD6xNFIhyrFiMD6wNFYh|ryP M4rN[VI2PDh5OUG3
MV4-11-ITD/F691L MoLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TEc2lEPTB;MD6xNVIhyrFiMD6wNVUh|ryP MmGxNlU1QDd7MUe=
MV4-11-ITD/N841K NWHITmFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvkPItQUUN3ME2wMlEyOyEEsTCwMlAxOiEQvF2= NF3ubnEzPTR6N{mxOy=>
U937-FLT3 WT MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmX5TWM2OD1yLkGwNkDDuSByLkCxN{DPxE1? MVSyOVQ5PzlzNx?=

... Click to View More Cell Line Experimental Data

体内研究 PD 0332991(150 mg/kg)作用于Colo-205结肠癌移植瘤,诱导肿瘤快速衰退,肿瘤生长相应延迟。PD 0332991(150 mg/kg)作用于MDA-MB-435乳腺癌,诱导全部肿瘤停滞和杀死细胞。PD 0332991(150 mg/kg)处理携带SF-295胶质母细胞瘤,和ZR-75-1乳腺癌和PC-3前列腺肿瘤模型(完全抑制肿瘤生长)的小鼠,显著诱导肿瘤衰退。PD 0332991 (150 mg/kg)处理 MDA-MB-435乳腺癌超过24小时,抑制Rb在Ser780位点磷酸化。PD 0332991(150 mg/kg)处理Colo-205 移植瘤,下调四种E2F调节的基因CDC2, CCNE2, TK1, 和 TOP2A表达。[1]PD 0332991也快速抑制骨髓瘤生长。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[4]
+ 展开

CDK活性实验:

在96孔过滤板中进行动力学测评,测定CDK实验的IC50值。所有的CDK-cyclin激酶复合物在昆虫细胞中通过杆状病毒感染而表达,并进行纯化。实验底物是与GST(GST•RB-Cterm)融合的pRb组分(792–928位氨基酸)。总反应体积为0.1 mL,包含终浓度20 mM Tris-HCl,pH 7.4, 50 mM NaCl,1 mM 二硫苏糖醇,10 mM MgCl2,含0.25 μCi[γ-32P]ATP的25 μM ATP(作用于 CDK4-cyclin D1, CDK6-cyclin D2, 和 CDK6-cyclin D3), 20 ng 酶, 1 μg GST•RB-Cterm, 及适度稀释的抑制剂。每孔加入全部组分,除了[γ-32P]ATP,置于混合器中2分钟。加入[γ-32P]ATP开始反应,在25°C下温育15分钟。加入0.1 mL 20% 三氯乙酸终止反应, 实验板置于4°C至少1小时,使底物沉淀。每孔使用 0.2 mL 10%三氯乙酸洗涤 五次,使用β计数器测定渗透的放射性。
细胞实验:[3]
+ 展开
  • Cell lines: 人类乳腺癌细胞MDA-MB-435
  • Concentrations: 2 μM
  • Incubation Time: 6 天
  • Method: 细胞按一式两份每孔5,000 到10,000个细胞接种在24孔板中,接种后,加入不同浓度的PD 0332991。对照组不加入药物。温育末期,细胞胰蛋白酶化,并置于等渗溶液中,并立即使用Coulter Z2粒子计数器计数。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 人类结肠癌移植瘤Colo-205
  • Formulation: 乳酸钠缓冲溶液(50 mM, pH 4.0)
  • Dosages: 150 mg/kg
  • Administration: 每天口服处理
    (Only for Reference)

溶解度 (25°C)

体外 Water 10 mg/mL warmed (17.43 mM)
DMSO Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
saline (with warming)
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 573.66
化学式

C24H29N7O2.C2H6O4S

CAS号 827022-33-3
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03709680 Not yet recruiting Solid Tumors|Ewing Sarcoma|Rhabdoid Tumor|Rhabdomyosarcoma|Neuroblastoma|Medulloblastoma Pfizer February 5 2019 Phase 1
NCT03609047 Not yet recruiting Breast Cancer Stage II|Breast Cancer Stage III European Organisation for Research and Treatment of Cancer - EORTC|Pfizer January 7 2019 Phase 2
NCT03691493 Not yet recruiting Anatomic Stage IV Breast Cancer AJCC v8|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Metastatic Malignant Neoplasm in the Bone|Progesterone Receptor Positive|Prognostic Stage IV Breast Cancer AJCC v8 Emory University|Pfizer December 1 2018 Phase 2
NCT03530696 Not yet recruiting HER2-positive Breast Cancer|Breast Cancer|Breast Cancer Stage|Recurrent Breast Cancer|Metastatic Breast Cancer|HER2 Positive Breast Carcinoma University of Arizona|Pfizer November 30 2018 Phase 2
NCT03531645 Not yet recruiting Malignant Neoplasms of Female Genital Organs M.D. Anderson Cancer Center|AstraZeneca|Pfizer November 2018 Phase 2
NCT03535506 Recruiting DCIS Georgetown University|Pfizer October 8 2018 Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

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

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CDK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID