WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H414744
CAS#: 135729-61-2 (free base)
Description: Palonosetron Free Base is an isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.
Hodoodo Cat#: H414744
Name: Palonosetron Free Base
CAS#: 135729-61-2 (free base)
Chemical Formula: C19H24N2O
Exact Mass: 296.19
Molecular Weight: 296.410
Elemental Analysis: C, 76.99; H, 8.16; N, 9.45; O, 5.40
Related CAS #: 135729-62-3 (HCl); 135729-61-2 (free base)
Synonym: Palonosetron Free Base; NSC743769; NSC-743769; NSC 743769; 2-Qhbiqo
IUPAC/Chemical Name: 1H-Benz(de)isoquinolin-1-one, 2-(1-azabicyclo(2.2.2)oct-3-yl)-2,3,3a,4,5,6-hexahydro-, (S-(R*,R*))-
InChi Key: CPZBLNMUGSZIPR-NVXWUHKLSA-N
InChi Code: InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1
SMILES Code: O=C1N([C@@H]2CN3CCC2CC3)C[C@]4([H])C5=C1C=CC=C5CCC4
Appearance: 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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 296.41 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.
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: | |
In vitro protocol: | |
In vivo protocol: |
1: Siddiqui MA, Scott LJ. Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. doi: 10.2165/00003495-200464100-00006. PMID: 15139789.
2: Yang LP, Scott LJ. Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000. PMID: 19852528.
3: Kovács G, Wachtel AE, Basharova EV, Spinelli T, Nicolas P, Kabickova E. Palonosetron versus ondansetron for prevention of chemotherapy-induced nausea and vomiting in paediatric patients with cancer receiving moderately or highly emetogenic chemotherapy: a randomised, phase 3, double-blind, double-dummy, non- inferiority study. Lancet Oncol. 2016 Mar;17(3):332-344. doi: 10.1016/S1470-2045(15)00520-3. Epub 2016 Jan 19. PMID: 26795844.
4: Keating GM. Netupitant/Palonosetron: A Review in the Prevention of Chemotherapy-Induced Nausea and Vomiting. Drugs. 2015 Dec;75(18):2131-41. doi: 10.1007/s40265-015-0512-9. PMID: 26613606.
5: Yang Y, Zhang L. A narrative review of tropisetron and palonosetron for the control of chemotherapy-induced nausea and vomiting. Chin Clin Oncol. 2020 Apr;9(2):17. doi: 10.21037/cco.2019.11.02. Epub 2019 Dec 16. PMID: 31865713.
6: Saito M, Aogi K, Sekine I, Yoshizawa H, Yanagita Y, Sakai H, Inoue K, Kitagawa C, Ogura T, Mitsuhashi S. Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, double-dummy, randomised, comparative phase III trial. Lancet Oncol. 2009 Feb;10(2):115-24. doi: 10.1016/S1470-2045(08)70313-9. Epub 2009 Jan 8. Erratum in: Lancet Oncol. 2010 Mar;11(3)226. PMID: 19135415.
7: Navari RM. Palonosetron for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother. 2014 Dec;15(17):2599-608. doi: 10.1517/14656566.2014.972366. Epub 2014 Oct 17. PMID: 25323946.
8: Singh PM, Borle A, Gouda D, Makkar JK, Arora MK, Trikha A, Sinha A, Goudra B. Efficacy of palonosetron in postoperative nausea and vomiting (PONV)-a meta- analysis. J Clin Anesth. 2016 Nov;34:459-82. doi: 10.1016/j.jclinane.2016.05.018. Epub 2016 Jun 28. Erratum in: J Clin Anesth. 2016 Dec;35:492. PMID: 27687434.
9: Pharmacoeconomic Review Report: Netupitant/Palonosetron 300 mg/0.5 mg (Akynzeo): (Purdue Pharma): Indication: In combination with dexamethasone, once- per-cycle treatment for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic cancer chemotherapy, or with moderately emetogenic cancer chemotherapy that is uncontrolled by a 5-HT3 receptor antagonist alone [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Jun. PMID: 30457774.
10: Navari RM. Palonosetron: a second generation 5-hydroxytryptamine 3 receptor antagonist. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1577-86. doi: 10.1517/17425250903407289. PMID: 19929251.