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MedKoo Cat#: 123215 | Name: Palbociclib free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

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

Theoretical Analysis

MedKoo Cat#: 123215

Name: Palbociclib free base

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

Chemical Formula: C24H29N7O2

Exact Mass: 447.2383

Molecular Weight: 447.54

Elemental Analysis: C, 64.41; H, 6.53; N, 21.91; O, 7.15

Price and Availability

Size Price Availability Quantity
100mg USD 150.00 Ready to ship
500mg USD 250.00 Ready to ship
1g USD 450.00 Ready to ship
2g USD 750.00 Ready to ship
5g USD 1,350.00 Ready to ship
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Related CAS #
571190-30-2 (free base) 827022-32-2 (HCl) 827022-33-3 (isethionate) Unknown (Palbociclib-SMCC) Unknown (Succinic)
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
Appearance
Yellow solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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).
HS Tariff Code
2934.99.9001
More Info
CAS# related to Palbociclib CAS#571190-30-2 (Palbociclib free base); CAS# 827022-32-2 ( PalbociclibHCl salt); CAS#827022-33-3 (Palbociclib Isethionate)
Biological target:
Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively.
In vitro activity:
This study aimed to explore the expression and function of CDC37L1 in gastric cancer (GC). To confirm whether CDC37L1 suppresses cell growth through decreasing CDK6 expression in GC, cell proliferation assays were performed after GC cells were treated with Palbociclib, an inhibitor of CDK4/6. Strikingly, Palbociclib significantly abolished the effects of CDC37L1 on cell growth in MGC-803 and BGC-823 cells (Figure6A). Similarly, CDC37L1 silencing increased the numbers of colonies compared with control, while there was no significant difference between the LvshCDC37L1 combined with Palbociclib group and the LvNC combined with Palbociclib group (Figure6B). In addition, flow cytometry analysis revealed that CDC37L1 knockdown led to much more cells in S phase of cell cycle, whereas this increase in S phase cells could be hindered by Palbociclib treatment (Figure6C). These results demonstrated that Palbociclib could inhibit CDC37L1 knockdown induced GC cell proliferation, further suggested the functional relevance between CDC37L1 and CDK6. J Cancer. 2021; 12(11): 3145–3153.https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8100790/
In vivo activity:
The objective of this study was to explore the effects of palbociclib (a CDK4/6 inhibitor) on inflammation in a lupus-prone MRL-lpr mouse model. Twenty mice (10 females and 10 males) were randomized into control group (n=10, treated with vehicle) and treatment group (n=10, treated with 3 cycles of palbociclib at a dose of 120 mg/kg/day for 2 weeks on and 10 weeks off, through oral gavage). Palbociclib treatment was able to reduce inflammation in the facial skin and lymph nodes, two main clinical features of lupus in the female mice. Splenomegaly was obvious in both female and male mice. However, palbociclib treatment did not inhibit the spleen enlargement. It was noted that palbociclib treatment slightly decreased the spleen weight of the female mice, but the decrease was not statistically significant. Palbociclib treatment was only able to inhibit nephritis in the male mice, but not the female mice. These findings suggest that palbociclib has certain gender-/organ-specific actions, the underlying mechanisms of which are unknown. Both female and male mice showed mild inflammatory cell infiltration in the lungs. Palbociclib treatment did not significantly reduce or increase the mild pulmonary inflammation. In conclusion, the findings suggest that palbociclib treatment reduces inflammation in lupus-prone mice in a gender-specific manner, targeting the facial skin and lymph nodes in the female mice and the kidneys in the male mice. Am J Clin Exp Urol. 2021; 9(1): 32–43. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8012823/
Solvent mg/mL mM
Solubility
DMSO (with a few drops of 5% HCl, pH = ~3) 25.0 55.86
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 447.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Li L, Tao X, Li Y, Gao Y, Li Q. CDC37L1 acts as a suppressor of migration and proliferation in gastric cancer by down-regulating CDK6. J Cancer. 2021 Mar 31;12(11):3145-3153. doi: 10.7150/jca.56097. PMID: 33976724; PMCID: PMC8100790. 2. Heckler M, Ali LR, Clancy-Thompson E, Qiang L, Ventre KS, Lenehan P, Roehle K, Luoma A, Boelaars K, Peters V, McCreary J, Boschert T, Wang ES, Suo S, Marangoni F, Mempel TR, Long HW, Wucherpfennig KW, Dougan M, Gray NS, Yuan GC, Goel S, Tolaney SM, Dougan SK. Inhibition of CDK4/6 promotes CD8 T-cell memory formation. Cancer Discov. 2021 May 3:candisc.1540.2020. doi: 10.1158/2159-8290.CD-20-1540. Epub ahead of print. PMID: 33941591. 3. Zhang Y, Jin B, Miller HD, Ge D, Zhang X, You Z. CDK4/6 inhibitor palbociclib reduces inflammation in lupus-prone mice. Am J Clin Exp Urol. 2021 Feb 15;9(1):32-43. PMID: 33816692; PMCID: PMC8012823 4. Guo C, Guo Y, Liu J, Gao Y, Wei M, Zhao R, Chen M, Zhang G. The G1 phase optical reporter serves as a sensor of CDK4/6 inhibition in vivo. Int J Biol Sci. 2021 Jan 31;17(3):728-741. doi: 10.7150/ijbs.52101. PMID: 33767584; PMCID: PMC7975702.
In vitro protocol:
1. Li L, Tao X, Li Y, Gao Y, Li Q. CDC37L1 acts as a suppressor of migration and proliferation in gastric cancer by down-regulating CDK6. J Cancer. 2021 Mar 31;12(11):3145-3153. doi: 10.7150/jca.56097. PMID: 33976724; PMCID: PMC8100790. 2. Heckler M, Ali LR, Clancy-Thompson E, Qiang L, Ventre KS, Lenehan P, Roehle K, Luoma A, Boelaars K, Peters V, McCreary J, Boschert T, Wang ES, Suo S, Marangoni F, Mempel TR, Long HW, Wucherpfennig KW, Dougan M, Gray NS, Yuan GC, Goel S, Tolaney SM, Dougan SK. Inhibition of CDK4/6 promotes CD8 T-cell memory formation. Cancer Discov. 2021 May 3:candisc.1540.2020. doi: 10.1158/2159-8290.CD-20-1540. Epub ahead of print. PMID: 33941591.
In vivo protocol:
1. Zhang Y, Jin B, Miller HD, Ge D, Zhang X, You Z. CDK4/6 inhibitor palbociclib reduces inflammation in lupus-prone mice. Am J Clin Exp Urol. 2021 Feb 15;9(1):32-43. PMID: 33816692; PMCID: PMC8012823 2. Guo C, Guo Y, Liu J, Gao Y, Wei M, Zhao R, Chen M, Zhang G. The G1 phase optical reporter serves as a sensor of CDK4/6 inhibition in vivo. Int J Biol Sci. 2021 Jan 31;17(3):728-741. doi: 10.7150/ijbs.52101. PMID: 33767584; PMCID: PMC7975702.
1: Wu J, Wang J, O'Connor TN, Tzetzo SL, Gurova KV, Knudsen ES, Witkiewicz AK. Separable cell cycle arrest and immune response elicited through pharmacological CDK4/6 and MEK inhibition in RASmut disease models. Mol Cancer Ther. 2024 Aug 16. doi: 10.1158/1535-7163.MCT-24-0369. Epub ahead of print. PMID: 39148328. 2: Fu JF, Hsu CL, Hsu PC. The antitumor activity of osimertinib plus palbociclib in non-small cell lung cancer patient-derived xenograft (PDX)/2D/3D culture models harboring EGFR amplification and CDKN2A/2B homozygous deletions. Neoplasia. 2024 Aug 14;57:101039. doi: 10.1016/j.neo.2024.101039. Epub ahead of print. PMID: 39146623. 3: Wen Y, Sun X, Zeng L, Liang S, Li D, Chen X, Zeng F, Zhang C, Wang Q, Zhong Q, Deng L, Guo L. CDK4/6 Inhibitors Impede Chemoresistance and Inhibit Tumor Growth of Small Cell Lung Cancer. Adv Sci (Weinh). 2024 Aug 13:e2400666. doi: 10.1002/advs.202400666. Epub ahead of print. PMID: 39136283. 4: Chen BF, Tsai YF, Chao TC, Lien PJ, Lin YS, Feng CJ, Chen YJ, Cheng HF, Liu CY, Lai JI, Tseng LM, Huang CC. Real-world experience with CDK4/6 inhibitors in hormone receptor-positive metastatic and recurrent breast cancer: findings from an Asian population. Clin Exp Med. 2024 Aug 12;24(1):185. doi: 10.1007/s10238-024-01458-1. PMID: 39133334; PMCID: PMC11319386. 5: Lin W, Zeng Y, Weng L, Yang J, Zhuang W. Comparative analysis of adverse events associated with CDK4/6 inhibitors based on FDA's adverse event reporting system: a case control pharmacovigilance study. BMC Pharmacol Toxicol. 2024 Aug 9;25(1):47. doi: 10.1186/s40360-024-00770-6. PMID: 39123221; PMCID: PMC11312934. 6: Beypınar İ, Demir H, Yaslıkaya Ş, Köşeci T, Demir B, Çolak G, Ağaoğlu AB, Şahbazlar M, Şancı PC, Çabuk D, Işık U, Şahin E, Coşkun A, Caner B, Aykut T, Artaç M, Duygulu ME, Sever N, Öksüz S, Turan N, Aykan MB, Tüzün EK, Uysal M, Uğurlu İ, Sakin A, Acar C, Özaşkın D, Şakalar T, Keskinkılıç M, Yavuzşen T, Köse N, Ertürk İ, Yıldırım N, Balçık OY, Alkan A, Selvi O, Erçin E, Ünal OÜ, Karaçin C. Efficacy of everolimus plus hormonal treatment after cyclin-dependent kinase inhibitor; real-life experience, A TOG study. Breast Cancer Res Treat. 2024 Aug 9. doi: 10.1007/s10549-024-07456-x. Epub ahead of print. PMID: 39123071. 7: Patil PH, Desai MP, Rao RR, Mutalik S, Puralae Channabasavaiah J. Strategy to Improve the Oral Pharmacokinetics of Cyclin-Dependent Kinase 4/6 Inhibitors: Enhancing Permeability and CYP450 Inhibition by a Natural Bioenhancer. AAPS PharmSciTech. 2024 Aug 8;25(6):181. doi: 10.1208/s12249-024-02899-3. PMID: 39117933. 8: Baziyar MA, Hosseini A, Jandel F. The role of palbociclib on the alterations in CDKN2, CCNE1, E2F3, MDM2 expressions as target genes of miR-141. PLoS One. 2024 Aug 8;19(8):e0306545. doi: 10.1371/journal.pone.0306545. PMID: 39116089; PMCID: PMC11309483. 9: Mehata AK, Bonlawar J, Tamang R, Malik AK, Setia A, Kumar S, Challa RR, Vallamkonda B, Koch B, Muthu MS. PLGA Nanoplatform for the Hypoxic Tumor Delivery: Folate Targeting, Therapy, and Ultrasound/Photoacoustic Imaging. ACS Appl Bio Mater. 2024 Aug 8. doi: 10.1021/acsabm.4c00853. Epub ahead of print. PMID: 39115968. 10: Tzoumpa S, Bejar C, Villette B, Louveau B, Zelek L, Martin A, Briard O, Bitout D, Caux F, Battistella M, Mourah S, Maubec E. Clinical benefit from palbociclib, letrozole and goserelin combination therapy for sweat gland carcinoma with neuroendocrine differentiation (SCAND). J Eur Acad Dermatol Venereol. 2024 Aug 8. doi: 10.1111/jdv.20276. Epub ahead of print. PMID: 39115046. 11: Elazzazy S, Al-Ziftawi NH, Mohamed Ibrahim MI, Bujassoum S, Hamad A. Comparative cost-effectiveness analysis of CDK4/6 inhibitors in the first-line treatment of HR-positive and HER2-negative advanced breast cancer: a Markov's model-based evaluation. Front Oncol. 2024 Jul 24;14:1413676. doi: 10.3389/fonc.2024.1413676. PMID: 39114308; PMCID: PMC11303311. 12: Yang H, Zhang X, Xu L, Zhou Y, Ma R, Chen H, Zhao S, Baatar M, Chen L, Deng X, Gu H, Wang X. Palbociclib-derived multifunctional molecules for lysosomal targeting and diagnostic-therapeutic integration. Future Med Chem. 2024 Jul 2;16(13):1287-1298. doi: 10.1080/17568919.2024.2347072. Epub 2024 May 22. PMID: 39109433; PMCID: PMC11318731. 13: Patil PH, Desai M, Birangal S, Gurupur GS, Rao M, Yadav A, Kurawattimath V, Chaudhari A, Sharma T, Pinjari J, Channabasavaiah JP. The Effect of Concomitant Administration of Proton Pump Inhibitors on the Pharmacokinetics of CDK4/6 Inhibitors in Rats: Implications for the Evaluation of Hepatic and Transporter- Mediated Drug-Drug Interactions. Eur J Drug Metab Pharmacokinet. 2024 Aug 6. doi: 10.1007/s13318-024-00909-0. Epub ahead of print. PMID: 39105991. 14: Vanni S, Miserocchi G, Gallo G, Fausti V, Gabellone S, Liverani C, Spadazzi C, Cocchi C, Calabrese C, De Luca G, Bassi M, Gessaroli M, Tomasetti N, Campobassi A, Pieri F, Ercolani G, Cavaliere D, Gurrieri L, Riva N, Recine F, Ibrahim T, Mercatali L, Jones R, De Vita A. Role of CDK4 as prognostic biomarker in Soft Tissue Sarcoma and synergistic effect of its inhibition in dedifferentiated liposarcoma sequential treatment. Exp Hematol Oncol. 2024 Aug 5;13(1):74. doi: 10.1186/s40164-024-00540-4. PMID: 39103896; PMCID: PMC11299298. 15: Rauthan A, Jain A, Singh M, Sendur MAN. Palbociclib in HR-Positive, HER2-Negative Advanced/Metastatic Breast Cancer: A Systematic Scoping Review of Real-World Evidence from Countries Outside of Western Regions that Are Underrepresented in Clinical Trials. Oncol Ther. 2024 Aug 2. doi: 10.1007/s40487-024-00295-2. Epub ahead of print. PMID: 39095679. 16: Álvarez Criado J, Zamora Auñon P, Martínez Marín V, GarcíaTrevijano Cabetas M, Collada Sánchez VL, Espinosa Arranz E, Romero-Garrido JA, Benedi-González J, Díaz Almirón M, Herrero Ambrosio A. Proton pump inhibitors decrease efficacy of palbociclib in patients with metastatic breast. J Oncol Pharm Pract. 2024 Aug 2:10781552241269677. doi: 10.1177/10781552241269677. Epub ahead of print. PMID: 39095042. 17: Sen A, Khan S, Rossetti S, Broege A, MacNeil I, DeLaForest A, Molden J, Davis L, Iversrud C, Seibel M, Kopher R, Schulz S, Laing L. Assessments of prostate cancer cell functions highlight differences between a pan-PI3K/mTOR inhibitor, gedatolisib, and single-node inhibitors of the PI3K/AKT/mTOR pathway. Mol Oncol. 2024 Aug 2. doi: 10.1002/1878-0261.13703. Epub ahead of print. PMID: 39092562. 18: Wang C, Hwang M, Paulson B, Mhandire D, Ozair S, O'Connor TL, Gandhi S, Attwood KM, Hertz DL, Goey AK. Potential association of SULT2A1 and ABCG2 variant alleles with increased risk for palbociclib toxicity. Pharmacogenomics. 2024 Aug 2:1-9. doi: 10.1080/14622416.2024.2380240. Epub ahead of print. PMID: 39092502. 19: Chen SH, Chen CH, Lin HC, Yeh SA, Hwang TL, Chen PJ. Drug repurposing of cyclin-dependent kinase inhibitors for neutrophilic acute respiratory distress syndrome and psoriasis. J Adv Res. 2024 Jul 31:S2090-1232(24)00310-2. doi: 10.1016/j.jare.2024.07.026. Epub ahead of print. PMID: 39089617. 20: Attwa MW, Abdelhameed AS, Kadi AA. An ultra-fast ultra-high-performance liquid chromatography-tandem mass spectrometry method for estimating the in vitro metabolic stability of palbociclib in human liver microsomes: In silico study for metabolic lability, absorption, distribution, metabolism, and excretion features, and DEREK alerts screening. J Sep Sci. 2024 Aug;47(15):e2400346. doi: 10.1002/jssc.202400346. PMID: 39087624.