Name: Palbociclib HCl
CAS#: 827022-32-2 (HCl)
Chemical Formula: C24H29N7O2
Exact Mass:
Molecular Weight: 483.99
Elemental Analysis: C, 59.56; H, 6.25; Cl, 7.33; N, 20.26; O, 6.61
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp: +8618653174435
Skype: willgutian
EOS Med Chem produce Palbociclib,PD-0332991, 827022-32-2 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Palbociclib,PD-0332991, 827022-32-2 Intermediates, EOS Med Chem have 8; Palbociclib,PD-0332991, 827022-32-2 Impurity we have 10, all from GMP, FDA plant.
Now Palbociclib,PD-0332991, 827022-32-2 DMF document is preparing.
Until 2016, Aug, Palbociclib,PD-0332991, 827022-32-2 more than produced 25kg API, 120kg Intermediates
Palbociclib Ibrance;PD-0332991;Palbociclib;; 571190-30-2(free base)
Palbociclib HCl Ibrance;PD-0332991;Palbociclib;PD-0332991 HCl; 827022-32-2(HCl)
Palbociclib Intermediates 1-(6-nitropyridin-3-yl)piperazine 775288-71-6
Palbociclib Intermediates tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate 571189-16-7
Palbociclib Intermediates 6-bromo-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one 1016636-76-2
Palbociclib Intermediates 5-bromo-2-chloro-N-cyclopentylpyrimidin-4-amine 733039-20-8
Palbociclib Intermediates 2-chloro-8-cyclopentyl-5-Methylpyrido[2,3-d]pyriMidin-7(8H)-one 1013916-37-4
Palbociclib Intermediates Tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate 571188-59-5
Palbociclib Intermediates Tert-butyl 4-(6-((6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate 571188-82-4
Palbociclib Intermediates Tert-butyl 4-(6-((6-(1-butoxyvinyl)-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate
Palbociclib Intermediates 6-bromo-8-cyclopentyl-5-methyl-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7(8H)-one 571188-81-3
Palbociclib Intermediates Ethyl 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carboxylate 211245-62-4
Palbociclib Intermediates (4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)methanol 211245-63-5
Palbociclib Intermediates 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carbaldehyde 211245-64-6
Palbociclib Intermediates 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethanol 362656-31-3
Palbociclib Intermediates 8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one 362656-23-3
Description: 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.
Synonym: PD 0332991; PD-0332991; PD0332991; PD0332991; PD332991; PD-332991; PD 332991; Palbociclib, brand name: Ibrance
IUPAC/Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
SMILES Code: O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5.[H]Cl
CAS# related to Palbociclib
CAS#571190-30-2 (Palbociclib free base);
CAS# 827022-32-2 ( PalbociclibHCl salt);
CAS#827022-33-3 (Palbociclib Isethionate)
1: L'Allemain G. [Doubling time of progression-free survival by palbociclib in metastatic breast cancer]. Bull Cancer. 2015 Apr;102(4):300. doi: 10.1016/j.bulcan.2015.02.011. French. PubMed PMID: 26042255.
2: Palbociclib Extends Survival in Advanced Breast Cancer. Cancer Discov. 2015 Jun 2. [Epub ahead of print] PubMed PMID: 26036642.
3: Turner NC, Ro J, André F, Loi S, Verma S, Iwata H, Harbeck N, Loibl S, Huang Bartlett C, Zhang K, Giorgetti C, Randolph S, Koehler M, Cristofanilli M. Palbociclib in Hormone-Receptor-Positive Advanced Breast Cancer. N Engl J Med. 2015 Jun 1. [Epub ahead of print] PubMed PMID: 26030518.
4: Niesvizky R, Badros AZ, Costa LJ, Ely SA, Singhal SB, Stadtmauer EA, Haideri NA, Yacoub A, Hess G, Lentzsch S, Spicka I, Chanan-Khan AA, Raab MS, Tarantolo S, Vij R, Zonder JA, Huang X, Jayabalan D, Di Liberto M, Huang X, Jiang Y, Kim ST, Randolph S, Chen-Kiang S. Phase 1/2 study of cyclin-dependent kinase (CDK)4/6 inhibitor palbociclib (PD-0332991) with bortezomib and dexamethasone in relapsed/refractory multiple myeloma. Leuk Lymphoma. 2015 May 15:1-9. [Epub ahead of print] PubMed PMID: 25813205.
5: Dhillon S. Palbociclib: first global approval. Drugs. 2015 Apr;75(5):543-51. doi: 10.1007/s40265-015-0379-9. PubMed PMID: 25792301.
6: Finn RS, Crown JP, Lang I, Boer K, Bondarenko IM, Kulyk SO, Ettl J, Patel R, Pinter T, Schmidt M, Shparyk Y, Thummala AR, Voytko NL, Fowst C, Huang X, Kim ST, Randolph S, Slamon DJ. 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. 2015 Jan;16(1):25-35. doi: 10.1016/S1470-2045(14)71159-3. Epub 2014 Dec 16. PubMed PMID: 25524798.
7: Vaughn DJ, Hwang WT, Lal P, Rosen MA, Gallagher M, O'Dwyer PJ. Phase 2 trial of the cyclin-dependent kinase 4/6 inhibitor palbociclib in patients with retinoblastoma protein-expressing germ cell tumors. Cancer. 2015 May 1;121(9):1463-8. doi: 10.1002/cncr.29213. Epub 2014 Dec 18. PubMed PMID: 25522918.
8: DeMichele A, Clark AS, Tan KS, Heitjan DF, Gramlich K, Gallagher M, Lal P, Feldman M, Zhang P, Colameco C, Lewis D, Langer M, Goodman N, Domchek S, Gogineni K, Rosen M, Fox K, O'Dwyer P. CDK 4/6 inhibitor palbociclib (PD0332991) in Rb+ advanced breast cancer: phase II activity, safety, and predictive biomarker assessment. Clin Cancer Res. 2015 Mar 1;21(5):995-1001. doi: 10.1158/1078-0432.CCR-14-2258. Epub 2014 Dec 11. PubMed PMID: 25501126.
9: Altenburg JD, Farag SS. The potential role of PD0332991 (Palbociclib) in the treatment of multiple myeloma. Expert Opin Investig Drugs. 2015 Feb;24(2):261-71. doi: 10.1517/13543784.2015.993753. Epub 2014 Dec 13. PubMed PMID: 25494820.
10: Schultz KA, Petronio J, Bendel A, Patterson R, Vaughn DJ. PD0332991 (Palbociclib) for treatment of pediatric intracranial growing teratoma syndrome. Pediatr Blood Cancer. 2015 Jun;62(6):1072-4. doi: 10.1002/pbc.25338. Epub 2014 Nov 21. PubMed PMID: 25417786.
11: de Melo-Diogo D, Gaspar VM, Costa EC, Moreira AF, Oppolzer D, Gallardo E, Correia IJ. Combinatorial delivery of Crizotinib-Palbociclib-Sildenafil using TPGS-PLA micelles for improved cancer treatment. Eur J Pharm Biopharm. 2014 Nov;88(3):718-29. doi: 10.1016/j.ejpb.2014.09.013. Epub 2014 Oct 13. PubMed PMID: 25308930.
12: Cadoo KA, Gucalp A, Traina TA. Palbociclib: an evidence-based review of its potential in the treatment of breast cancer. Breast Cancer (Dove Med Press). 2014 Aug 4;6:123-33. doi: 10.2147/BCTT.S46725. eCollection 2014. Review. PubMed PMID: 25177151; PubMed Central PMCID: PMC4128689.
13: Pauls E, Badia R, Torres-Torronteras J, Ruiz A, Permanyer M, Riveira-Muñoz E, Clotet B, Marti R, Ballana E, Esté JA. Palbociclib, a selective inhibitor of cyclin-dependent kinase4/6, blocks HIV-1 reverse transcription through the control of sterile α motif and HD domain-containing protein-1 (SAMHD1) activity. AIDS. 2014 Sep 24;28(15):2213-22. doi: 10.1097/QAD.0000000000000399. PubMed PMID: 25036183.
14: Palbociclib ups PFS in HER2-/ER+ breast cancer. Cancer Discov. 2014 Jun;4(6):624-5. doi: 10.1158/2159-8290.CD-NB2014-053. Epub 2014 Apr 6. PubMed PMID: 24891344.
15: Rocca A, Farolfi A, Bravaccini S, Schirone A, Amadori D. Palbociclib (PD 0332991) : targeting the cell cycle machinery in breast cancer. Expert Opin Pharmacother. 2014 Feb;15(3):407-20. doi: 10.1517/14656566.2014.870555. Epub 2013 Dec 26. Review. PubMed PMID: 24369047.
