Palbociclib free base
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MedKoo CAT#: 123215

CAS#: 571190-30-2 (free base)

Description: 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.


Price and Availability

Size
Price

100mg
USD 150
5g
USD 1650
Size
Price

500mg
USD 450
10g
USD 2650
Size
Price

1g
USD 650
50g
USD 5650

Palbociclib free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 123215
Name: Palbociclib free base
CAS#: 571190-30-2 (free base)
Chemical Formula: C24H29N7O2
Exact Mass: 447.23827
Molecular Weight: 447.543
Elemental Analysis: C, 64.41; H, 6.53; N, 21.91; O, 7.15


Related CAS #: 571190-30-2 (free base)   827022-32-2 (HCl)   827022-33-3 (isethionate)   Unknown (Palbociclib-SMCC)    

Synonym: PD-0332991; PD 0332991; PD0332991; Palbociclib free base, 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

InChi Key: AHJRHEGDXFFMBM-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5


Technical Data

Appearance:
Yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

CAS# related to Palbociclib
CAS#571190-30-2 (Palbociclib free base);
CAS# 827022-32-2 ( PalbociclibHCl salt);
CAS#827022-33-3 (Palbociclib Isethionate)


References

1: Badia R, Angulo G, Riveira-Muñoz E, Pujantell M, Puig T, Ramirez C, Torres-Torronteras J, Martí R, Pauls E, Clotet B, Ballana E, Esté JA. Inhibition of herpes simplex virus type 1 by the CDK6 inhibitor PD-0332991 (palbociclib) through the control of SAMHD1. J Antimicrob Chemother. 2015 Nov 4. pii: dkv363. [Epub ahead of print] PubMed PMID: 26542306.

2: Qin G, Xu F, Qin T, Zheng Q, Shi D, Xia W, Tian Y, Tang Y, Wang J, Xiao X, Deng W, Wang S. Palbociclib inhibits epithelial-mesenchymal transition and metastasis in breast cancer via c-Jun/COX-2 signaling pathway. Oncotarget. 2015 Oct 19. doi: 10.18632/oncotarget.5993. [Epub ahead of print] PubMed PMID: 26540629.

3: Ozaki A, Tanimoto T, Saji S. Palbociclib in Hormone-Receptor-Positive Advanced Breast Cancer. N Engl J Med. 2015 Oct 22;373(17):1672-3. doi: 10.1056/NEJMc1510345#SA1. PubMed PMID: 26488701.

4: Turner NC, Huang Bartlett C, Cristofanilli M. Palbociclib in Hormone-Receptor-Positive Advanced Breast Cancer. N Engl J Med. 2015 Oct 22;373(17):1672-3. doi: 10.1056/NEJMc1510345. PubMed PMID: 26488700.

5: Solimando DA Jr, Waddell JA. Lenvatinib and Palbociclib. Hosp Pharm. 2015 Jul;50(7):578-82. doi: 10.1310/hpj5007-578. Epub 2015 Jul 31. PubMed PMID: 26448668; PubMed Central PMCID: PMC4589862.

6: Palbociclib Prolongs Progression-Free Survival in Patients with Advanced Breast Cancer. Am Health Drug Benefits. 2015 Aug;8(Spec Issue):36. PubMed PMID: 26380621; PubMed Central PMCID: PMC4570077.

7: Parrish KE, Pokorny J, Mittapalli RK, Bakken K, Sarkaria JN, Elmquist WF. Efflux Transporters at the Blood-Brain Barrier Limit Delivery and Efficacy of Cyclin-Dependent Kinase 4/6 Inhibitor Palbociclib (PD-0332991) in an Orthotopic Brain Tumor Model. J Pharmacol Exp Ther. 2015 Nov;355(2):264-71. doi: 10.1124/jpet.115.228213. Epub 2015 Sep 9. PubMed PMID: 26354993; PubMed Central PMCID: PMC4613960.

8: Beaver JA, Amiri-Kordestani L, Charlab R, Chen W, Palmby T, Tilley A, Zirkelbach JF, Yu J, Liu Q, Zhao L, Crich J, Chen XH, Hughes M, Bloomquist E, Tang S, Sridhara R, Kluetz PG, Kim G, Ibrahim A, Pazdur R, Cortazar P. FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer. Clin Cancer Res. 2015 Nov 1;21(21):4760-6. doi: 10.1158/1078-0432.CCR-15-1185. Epub 2015 Aug 31. PubMed PMID: 26324739.

9: Mangini NS, Wesolowski R, Ramaswamy B, Lustberg MB, Berger MJ. Palbociclib: A Novel Cyclin-Dependent Kinase Inhibitor for Hormone Receptor-Positive Advanced Breast Cancer. Ann Pharmacother. 2015 Nov;49(11):1252-60. doi: 10.1177/1060028015602273. Epub 2015 Aug 31. Review. PubMed PMID: 26324355.

10: Lu J. Palbociclib: a first-in-class CDK4/CDK6 inhibitor for the treatment of hormone-receptor positive advanced breast cancer. J Hematol Oncol. 2015 Aug 13;8:98. doi: 10.1186/s13045-015-0194-5. PubMed PMID: 26264704; PubMed Central PMCID: PMC4534142.

11: Palbociclib (Ibrance) for metastatic breast cancer. Med Lett Drugs Ther. 2015 Aug 17;57(1475):115-6. PubMed PMID: 26262882.

12: McCain J. First-in-Class CDK4/6 Inhibitor Palbociclib Could Usher in a New Wave of Combination Therapies for HR+, HER2- Breast Cancer. P T. 2015 Aug;40(8):511-20. PubMed PMID: 26236140; PubMed Central PMCID: PMC4517534.

13: Carey LA, Perou CM. Palbociclib--Taking Breast-Cancer Cells Out of Gear. N Engl J Med. 2015 Jul 16;373(3):273-4. doi: 10.1056/NEJMe1506680. PubMed PMID: 26176385.

14: de Gooijer MC, Zhang P, Thota N, Mayayo-Peralta I, Buil LC, Beijnen JH, van Tellingen O. P-glycoprotein and breast cancer resistance protein restrict the brain penetration of the CDK4/6 inhibitor palbociclib. Invest New Drugs. 2015 Oct;33(5):1012-9. doi: 10.1007/s10637-015-0266-y. Epub 2015 Jul 1. PubMed PMID: 26123925.

15: Morikawa A, Henry NL. Palbociclib for the Treatment of Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer. Clin Cancer Res. 2015 Aug 15;21(16):3591-6. doi: 10.1158/1078-0432.CCR-15-0390. Epub 2015 Jun 22. PubMed PMID: 26100274; PubMed Central PMCID: PMC4537809.

16: Harding E. Palbociclib for hormone receptor-positive breast cancer. Lancet Oncol. 2015 Jul;16(7):e318. doi: 10.1016/S1470-2045(15)00032-7. Epub 2015 Jun 7. PubMed PMID: 26062777.

17: 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.

18: Palbociclib Extends Survival in Advanced Breast Cancer. Cancer Discov. 2015 Jul;5(7):OF5. doi: 10.1158/2159-8290.CD-NB2015-083. Epub 2015 Jun 2. PubMed PMID: 26036642.

19: 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; PALOMA3 Study Group. Palbociclib in Hormone-Receptor-Positive Advanced Breast Cancer. N Engl J Med. 2015 Jul 16;373(3):209-19. doi: 10.1056/NEJMoa1505270. Epub 2015 Jun 1. PubMed PMID: 26030518.

20: 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.