Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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P126849-10mg | 10mg | In stock | $82.90 | |
P126849-50mg | 50mg | In stock | $105.90 | |
P126849-100mg | 100mg | In stock | $129.90 | |
P126849-500mg | 500mg | In stock | $307.90 |
Potent, highly specific Cdk4/Cdk6\xa0inhibitor
Synonyms | PD0332991 | PD991 | PF 00080665 | PF-00080665 | PF00080665 | 6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | Palbociclib- Bio-X | palbociclibum | R 802 (bactericide) | SY026143 | 6-ACETYL-8-CYCLOPEN |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4) (IC50, 0.011 μmol/L) |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Cyclin-dependent kinase 4/cyclin D1 inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. |
ALogP | 1.8 |
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Pubchem Sid | 488195370 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488195370 |
IUPAC Name | 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-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) |
InChi Key | AHJRHEGDXFFMBM-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C |
Isomeric SMILES | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C |
Alternate CAS | 571190-30-2 |
PubChem CID | 5330286 |
MeSH Entry Terms | 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-8H-pyrido(2,3-d)pyrimidin-7-one;Ibrance;palbociclib;PD 0332991;PD-0332991;PD0332991 |
Molecular Weight | 447.53 |
ChEMBL Ligand | CHEMBL189963 |
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PubChem CID | 5330286 |
CAS Registry No. | 571190-30-2 |
Wikipedia | Palbociclib |
RCSB PDB Ligand | LQQ |
PEP | palbociclib |
DrugCentral Ligand | 4941 |
PubChem SID | 488195370 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
D2303098 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2312478 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2312486 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2312487 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2312488 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2313084 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2313087 | Certificate of Analysis | Mar 13, 2023 | P126849 |
D2313097 | Certificate of Analysis | Mar 13, 2023 | P126849 |
Solubility | DMSO |
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Pictogram(s) | GHS06, GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H301:Toxic if swallowed H341:Suspected of causing genetic defects H373:Causes damage to organs through prolonged or repeated exposure H411:Toxic to aquatic life with long lasting effects H302:Harmful if swallowed H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P281:Use personal protective equipment as required. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
1. Huiling Zhou, Chenxin Duan, Huimin Qin, Chaonan Huang, Jingxuan Hou, Yanming Chen, Jin Zhu, Cangcang Xu, Jian Jin, Tao Zhuang. (2023) Synthesis and structural characterization of a novel palbociclib-kaempferol cocrystal with improved tabletability and synergistic antitumor activity. JOURNAL OF MOLECULAR STRUCTURE, 1281 (135101). [PMID:] |
2. Li Tian, Zhou An-Di, Bai Li-Fei, Zhang Xiao-Yang, Zhou Yu-Ting, Yang Hai-Li, Xu Le-Tian, Guo Xin-Qin, Zhu Xi-Yu, Wang Dong-Jin, Gu Hong-Wei, Wang Xiao-Ming. (2022) Design, synthesis, and anticancer activity of three novel palbociclib derivatives. Frontiers in Oncology, 12 [PMID:36091173] |
3. Chenxin Duan, Wenwen Liu, Yunwen Tao, Feifei Liang, Yanming Chen, Xinyi Xiao, Guisen Zhang, Yin Chen, Chao Hao. (2022) Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate. Pharmaceutics, 14 (1): (23). [PMID:35056919] |
1. Wang L, Wang J, Blaser BW, Duchemin AM, Kusewitt DF, Liu T, Caligiuri MA, Briesewitz R. (2007) Pharmacologic inhibition of CDK4/6: mechanistic evidence for selective activity or acquired resistance in acute myeloid leukemia.. Blood, 110 (6): (2075-83). [PMID:17537993] |
2. Finn RS, Dering J, Conklin D, Kalous O, Cohen DJ, Desai AJ, Ginther C, Atefi M, Chen I, Fowst C et al.. (2009) PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro.. Breast Cancer Res, 11 (5): (R77). [PMID:19874578] |
3. Fry DW, Harvey PJ, Keller PR, Elliott WL, Meade M, Trachet E, Albassam M, Zheng X, Leopold WR, Pryer NK et al.. (2004) Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts.. Mol Cancer Ther, 3 (11): (1427-38). [PMID:15542782] |
4. Toogood PL, Harvey PJ, Repine JT, Sheehan DJ, VanderWel SN, Zhou H, Keller PR, McNamara DJ, Sherry D, Zhu T et al.. (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.. J Med Chem, 48 (7): (2388-406). [PMID:15801831] |
5. Beroukhim R, Mermel CH, Porter D, Wei G, Raychaudhuri S, Donovan J, Barretina J, Boehm JS, Dobson J, Urashima M et al.. (2010) The landscape of somatic copy-number alteration across human cancers.. Nature, 463 (7283): (899-905). [PMID:20164920] |
6. Wiedemeyer WR, Dunn IF, Quayle SN, Zhang J, Chheda MG, Dunn GP, Zhuang L, Rosenbluh J, Chen S, Xiao Y et al.. (2010) Pattern of retinoblastoma pathway inactivation dictates response to CDK4/6 inhibition in GBM.. Proc Natl Acad Sci USA, 107 (25): (11501-6). [PMID:20534551] |
7. Puyol M, Martín A, Dubus P, Mulero F, Pizcueta P, Khan G, Guerra C, Santamaría D, Barbacid M. (2010) A synthetic lethal interaction between K-Ras oncogenes and Cdk4 unveils a therapeutic strategy for non-small cell lung carcinoma.. Cancer Cell, 18 (1): (63-73). [PMID:20609353] |
8. Dean JL, McClendon AK, Hickey TE, Butler LM, Tilley WD, Witkiewicz AK, Knudsen ES. (2012) Therapeutic response to CDK4/6 inhibition in breast cancer defined by ex vivo analyses of human tumors.. Cell Cycle, 11 (14): (2756-61). [PMID:22767154] |
9. Choi YJ, Li X, Hydbring P, Sanda T, Stefano J, Christie AL, Signoretti S, Look AT, Kung AL, von Boehmer H et al.. (2012) The requirement for cyclin D function in tumor maintenance.. Cancer Cell, 22 (4): (438-51). [PMID:23079655] |
10. Sawai CM, Freund J, Oh P, Ndiaye-Lobry D, Bretz JC, Strikoudis A, Genesca L, Trimarchi T, Kelliher MA, Clark M et al.. (2012) Therapeutic targeting of the cyclin D3:CDK4/6 complex in T cell leukemia.. Cancer Cell, 22 (4): (452-65). [PMID:23079656] |
11. Zhang XH, Cheng Y, Shin JY, Kim JO, Oh JE, Kang JH. (2013) A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS.. Cancer Biol Ther, 14 (7): (597-605). [PMID:23792647] |
12. Zanardi E, Bregni G, de Braud F, Di Cosimo S. (2015) Better Together: Targeted Combination Therapies in Breast Cancer.. Semin Oncol, 42 (6): (887-95). [PMID:26615133] |
13. Finn RS, Crown JP, Lang I, Boer K, Bondarenko IM, Kulyk SO, Ettl J, Patel R, Pinter T, Schmidt M et al.. (2015) The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study.. Lancet Oncol, 16 (1): (25-35). [PMID:25524798] |
14. Johnston SR. (2015) Enhancing Endocrine Therapy for Hormone Receptor-Positive Advanced Breast Cancer: Cotargeting Signaling Pathways.. J Natl Cancer Inst, 107 (10): (589-97). [PMID:26251289] |
15. Beaver JA, Amiri-Kordestani L, Charlab R, Chen W, Palmby T, Tilley A, Zirkelbach JF, Yu J, Liu Q, Zhao L et al.. (2015) FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer.. Clin Cancer Res, 21 (21): (4760-6). [PMID:26324739] |
16. Porter B. (1983) Primary care pediatrics vs. family practice: a nonissue.. Isr J Med Sci, 19 (8): (736-8). [PMID:6885367] |
17. Huiling Zhou, Chenxin Duan, Huimin Qin, Chaonan Huang, Jingxuan Hou, Yanming Chen, Jin Zhu, Cangcang Xu, Jian Jin, Tao Zhuang. (2023) Synthesis and structural characterization of a novel palbociclib-kaempferol cocrystal with improved tabletability and synergistic antitumor activity. JOURNAL OF MOLECULAR STRUCTURE, 1281 (135101). [PMID:] |
18. Li Tian, Zhou An-Di, Bai Li-Fei, Zhang Xiao-Yang, Zhou Yu-Ting, Yang Hai-Li, Xu Le-Tian, Guo Xin-Qin, Zhu Xi-Yu, Wang Dong-Jin, Gu Hong-Wei, Wang Xiao-Ming. (2022) Design, synthesis, and anticancer activity of three novel palbociclib derivatives. Frontiers in Oncology, 12 [PMID:36091173] |
19. Chenxin Duan, Wenwen Liu, Yunwen Tao, Feifei Liang, Yanming Chen, Xinyi Xiao, Guisen Zhang, Yin Chen, Chao Hao. (2022) Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate. Pharmaceutics, 14 (1): (23). [PMID:35056919] |