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827022-33-3 (Palbociclib (isethionate))

1

Identification

Palbociclib (isethionate) Palbociclib (isethionate)
Name Palbociclib (isethionate)
Formula C26H35N7O6S
MW 573.66
CAS No. 827022-33-3
EINECS
Smiles CC(C1=C(N2C3CCCC3)N=C(NC4=NC=C(N5CCNCC5)C=C4)N=C1)=C(C(C)=O)C2=O.OCCS(O)(=O)=O
Synonyms PD0332991 isethionate;PD-0332991 isethionate;PD 0332991 isethionate; 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one 2-hydroxyethanesulfonate
InChI InChI=1S/C24H29N7O2.C2H6O4S/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;3-1-2-7(4,5)6/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29);3H,1-2H2,(H,4,5,6)
2

Introduction

Palbociclib isethionate(PD-0332991 isethionate) 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

A potent and highly selective cyclindependent kinase 4 and 6 (CDK 4 and 6) ......by AOBIOUS INC
Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 2/3. ......by AbMole BioScience
PD 0332991 Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM respectively. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Palbociclib is a potent Cdk4/6 inhibitor. ......by BOC Sciences
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 (isethionate) is a highly selective inhibitor of CDK4/6 with IC50s of 11 nM/16 nM, and shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc.  ......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. Isethionate was approved on 2/3/2015 for treatment of advanced (metastatic) breast cancer. ......by MedKoo Biosciences, Inc.
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. ......by Selleck Chemicals LLC
Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. ......by Target Molecule Corp.
Potent Cdk4/6 inhibitor (IC50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10 μM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000010557

Storage condition

Solubility

DMSO <1 mg/mL (<1 mM) ; Water 100 mg/mL (174 mM) ; Ethanol <1 mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

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

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD15() USA
AbMole BioScience 10mg/USD120(In stock) USA
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC 10mg/USD103(In stock) USA
Ark Pharm, Inc. USA
Axon Medchem BV 10mg/USD162(In Stock) Netherlands
BOC Sciences 250mg/USD188(In stock)
BioVision, Inc., 5mg/USD115() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD60();10mg/USD84() USA
ChemieTek 10mg/USD100() 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
Santa Cruz Biotechnology, Inc. 1mg/USD220() USA
Selleck Chemicals LLC 10mg/USD147(In stock);25mg/USD270(In stock);50mg/USD370(In stock);200mg/USD1070(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD60();10mg/USD84() China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD600(In stock) CHINA
Sigma-Aldrich, Inc. 5mg/USD86() USA
Target Molecule Corp. 10mg/USD125();25mg/USD198();50mg/USD352() USA
Tocris Bioscience Inc. 10mg/USD215() USA
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Related Products

Other Forms of 827022-33-3

Name CAS No Formula MW
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Palbociclib 571190-30-2 C24H29N7O2 447.53

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
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
NU6102 444722-95-6 C18H22N6O3S 402.47

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
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Route of Synthesis

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References

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More Information

Palbociclib (isethionate)

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