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571190-30-2 (Palbociclib)

1

Identification

Palbociclib Palbociclib
Name Palbociclib
Formula C24H29N7O2
MW 447.53
CAS No. 571190-30-2
EINECS
Smiles O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C
Synonyms PD0332991;PD-0332991;PD 0332991; 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
InChI InChI=1S/C24H29N7O2/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29)
2

Introduction

Palbociclib(PD-0332991) is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases. IC50 value: 11 nM/16 nM (Cdk4/Cdk6) [1] Target: Cdk4/Cdk6 in vitro: ATP competitive inhibitor of Cdk4.

Background Information

An orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases ......by AOBIOUS INC
PD 0332991 is an orally active, highly selective inhibitor of the cyclin D kinases (CDK)4 and CDK6 with ability to block retinoblastoma (Rb) phosphorylation in the low nanomolar range. PD-0332991 selectively inhibits cyclin-dependent kinases (particularly Cdk4/cyclin D1 kinase), which may inhibit retinoblastoma (Rb) protein phosphorylation; inhibition of Rb phosphorylation prevents Rb-positive tumor cells from entering the S phase of the cell cycle (arrest in the G1 phase), resulting in suppression of DNA replication and decreased tumor cell proliferation. PD 0332991 was synergistic with tamoxifen and trastuzumab in ER+ and HER2-amplified cell lines, respectively. PD 0332991 enhanced sensitivity to tamoxifen in cell lines with conditioned resistance to ER blockade. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F. The results indicate that inhibition of Cdk4/6 alone is sufficient to cause tumor regression and a net reduction in tumor burden in some tumors. ......by AbMole BioScience
Palbociclib is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. ......by AdooQ BioScience, LLC
PD 0332991 HCl is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Description ......by Apexbio Technology LLC
PD0332991 is a highly specific inhibitor of Cdk4 (IC₅₀ = 11 nM) and Cdk6 (IC₅₀ = 16 nM). Displays selectivity for Cdk4/6 over a panel of 34 additional protein kinases (IC₅₀ values are > 10 μM). ......by BioVision, Inc.,
Palbociclib is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases. ......by MedChemexpress Co., Ltd.
Palbociclib, also known as PD0332991, is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. PD-0332991 selectively inhibits cyclin-dependent kinases (particularly Cdk4/cyclin D1 kinase), which may inhibit retinoblastoma (Rb) protein phosphorylation; inhibition of Rb phosphorylation prevents Rb-positive tumor cells from entering the S phase of the cell cycle (arrest in the G1 phase), resulting in suppression of DNA replication and decreased tumor cell proliferation. PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) (IC50 = 0.011 μmol/L) and Cdk6 (IC50 = 0.016 μmol/L), having no activity against a panel of 36 additional protein kinases. Palbociclib was approved on 2/3/2015 for treatment of advanced (metastatic) breast cancer. ......by MedKoo Biosciences, Inc.
Palbociclib, also known as PD-0332991, is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of cell cycle progression. Palbociclib, was approved on February 3, 2015 as a treatment (in combination with letrozole) for patients with estrogen receptor-positive advanced breast cancer. ......by MedKoo Biosciences, Inc.
A potent and selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM; no inhibition for CDK2A (IC50>5 uM); inhibits MDA-MB453 cells with IC50 of 0.16 uM; shows antiproliferative effect against retinoblastoma (Rb)-positive tumor cells in vitro and reduces the phospho-Ser780/Ser795 on the Rb protein; orally bioavailable.Breast CancerApproved ......by ProbeChem
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. ......by Selleck Chemicals LLC
Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:yellow Solid EBNumber:EB000029146

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

<0.1 mg/ml in DMSO by CHEMSCENE, LLC
<0.1 mg/ml in DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Palbociclib Pfizer Inc Metastatic breast cancer 2013/9/30 2017/1/31 Phase 3 Clinical
Palbociclib German Breast Group Breast tumor 2013/10/31 2021/11/30 Phase 3 Clinical
Palbociclib Pfizer Inc Metastatic breast cancer 2013/2/28 2015/3/31 Phase 3 Clinical
Palbociclib Institut Bergonie Gastrointestinal stromal tumor 2013/8/31 2015/8/31 Phase 2 Clinical
Palbociclib Washington University in St Louis Breast tumor 2013/6/30 2015/8/31 Phase 2 Clinical
Palbociclib - Launched
7

Safety Data of Palbociclib

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD11() USA
AbMole BioScience USA
AdooQ BioScience, LLC USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
Ark Pharm, Inc. USA
BOC Sciences
Beijing Lunarsun Pharmaceutical Co., Ltd. China
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD60();10mg/USD84() USA
Cayman Chemical Company USA
LC Laboratoies 10mg/USD47(In stock);25mg/USD64(In stock);50mg/USD87(In stock);100mg/USD139(In stock);200mg/USD235(In stock);500mg/USD484(In stock);1g/USD792(In stock);2g/USD1384(In stock) USA
MedChemexpress Co., Ltd. 5mg/USD60();10mg/USD84() USA
MedKoo Biosciences, Inc. USA
MedKoo Biosciences, Inc. USA
ProbeChem
Pure Chemistry Scientific Inc. 10mg/USD156(In stock) USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD60();10mg/USD84() China
Shanghai Sun-shine Chemical Technology Co., Ltd. China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD400(In stock) CHINA
Target Molecule Corp. 10mg/USD76();50mg/USD223();100mg/USD369() USA
10

Related Products

Other Forms of 571190-30-2

Name CAS No Formula MW
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
Regorafenib 755037-03-7 C21H15ClF4N4O3 482.82
Ostarine 841205-47-8 C19H14F3N3O3 389.33
Toremifene 89778-26-7 C26H28ClNO 405.96
Toremifene (Citrate) 89778-27-8 C32H36ClNO8 598.08
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 261.09
Linsitinib 867160-71-2 C26H23N5O 421.49
Fenretinide 65646-68-6 C26H33NO2 391.55
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
Litronesib 910634-41-2 C23H37N5O4S2 511.701
Veliparib 912444-00-9 C13H16N4O 244.29
Veliparib (dihydrochloride) 912445-05-7 C13H18Cl2N4O 317.21
AT13387 912999-49-6 C24H31N3O3 409.52
Ganetespib 888216-25-9 C20H20N4O3 364.4
Ixabepilone 219989-84-1 C27H42N2O5S 506.7
Imatinib (Mesylate) 220127-57-1 C30H35N7O4S 589.71
Reparixin 266359-83-5 C14H21NO3S 283.39
Reparixin (L-lysine salt) 266359-93-7 C20H35N3O5S 429.57
11

Route of Synthesis

12

References

13

More Information

Palbociclib

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