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MedKoo Cat#: 565758 | Name: Copanlisib HCl hydrate

Description:

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

Copanlisib Dihydrochloride is a novel phosphoinositide 3-kinase (pi3k) inhibitor, inhibiting the activation of the pi3k signaling pathway, resulting in inhibition of tumor cell growth and survival in susceptible tumor cell populations

Chemical Structure

Copanlisib HCl hydrate
Copanlisib HCl hydrate
CAS#1402152-46-8 (HCl hydrate)

Theoretical Analysis

MedKoo Cat#: 565758

Name: Copanlisib HCl hydrate

CAS#: 1402152-46-8 (HCl hydrate)

Chemical Formula: C23H38Cl2N8O8

Exact Mass:

Molecular Weight: 625.51

Elemental Analysis: C, 44.16; H, 6.12; Cl, 11.33; N, 17.91; O, 20.46

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1402152-13-9 (HCl) 1032568-63-0 (free base) 1402152-46-8 (HCl hydrate)
Synonym
Copanlisib HCl; Copanlisib dihydrochloride; BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; Copanlisib HCl hydrate; trade name Aliqopa.
IUPAC/Chemical Name
5-Pyrimidinecarboxamide, 2-amino-N-(2,3-dihydro-7-methoxy-8-(3-(4-morpholinyl)propoxy)imidazo(1,2-C)quinazolin-5-yl)-, hydrochloride, hydrate (1:2:4)
InChi Key
PRZNRMHJLYLVBJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H28N8O4.2ClH.4H2O/c1-33-19-17(35-10-2-6-30-8-11-34-12-9-30)4-3-16-18(19)28-23(31-7-5-25-20(16)31)29-21(32)15-13-26-22(24)27-14-15;;;;;;/h3-4,13-14H,2,5-12H2,1H3,(H2,24,26,27)(H,28,29,32);2*1H;4*1H2
SMILES Code
O=C(C1=CN=C(N)N=C1)NC2=NC3=C(C=CC(OCCCN4CCOCC4)=C3OC)C5=NCCN25.[H]Cl.[H]Cl.[H]O[H].[H]O[H].[H]O[H].[H]O[H]
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
Soluble in DMSO
Shelf Life
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 625.51 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
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Cell Death Discov. 2019 Apr 5;5:86. doi: 10.1038/s41420-019-0165-7. eCollection 2019. PubMed PMID: 30962952; PubMed Central PMCID: PMC6450909. 4: Eltantawy A, Vallejos X, Sebea E, Evans K. Copanlisib: An Intravenous Phosphatidylinositol 3-Kinase (PI3K) Inhibitor for the Treatment of Relapsed Follicular Lymphoma. Ann Pharmacother. 2019 Sep;53(9):954-958. doi: 10.1177/1060028019833992. Epub 2019 Feb 27. PubMed PMID: 30813760. 5: Appukkuttan S, Duchesneau E, Zichlin ML, Bhak RH, Yaldo A, Gharibo M, Babajanyan S, Duh MS. A Budget Impact Analysis of the Introduction of Copanlisib for Treatment of Relapsed Follicular Lymphoma in the United States. J Manag Care Spec Pharm. 2019 Jan 4:1-12. doi: 10.18553/jmcp.2019.18259. [Epub ahead of print] PubMed PMID: 30608008. 6: Cheson BD, O'Brien S, Ewer MS, Goncalves MD, Farooki A, Lenz G, Yu A, Fisher RI, Zinzani PL, Dreyling M. Optimal Management of Adverse Events From Copanlisib in the Treatment of Patients With Non-Hodgkin Lymphomas. Clin Lymphoma Myeloma Leuk. 2019 Mar;19(3):135-141. doi: 10.1016/j.clml.2018.11.021. Epub 2018 Nov 29. PubMed PMID: 30584024; PubMed Central PMCID: PMC6642803. 7: Dittakavi S, Mullangi R. LC-ESI-MS/MS determination of copanlisib, a novel PI3K inhibitor, in mouse plasma and its application to a pharmacokinetic study in mice. Biomed Chromatogr. 2019 Apr;33(4):e4460. doi: 10.1002/bmc.4460. Epub 2019 Jan 7. PubMed PMID: 30536684. 8: Okabe S, Tanaka Y, Tauchi T, Ohyashiki K. Copanlisib, a novel phosphoinositide 3-kinase inhibitor, combined with carfilzomib inhibits multiple myeloma cell proliferation. Ann Hematol. 2019 Mar;98(3):723-733. doi: 10.1007/s00277-018-3547-7. Epub 2018 Nov 15. PubMed PMID: 30430191. 9: Krause G, Hassenrück F, Hallek M. Copanlisib for treatment of B-cell malignancies: the development of a PI3K inhibitor with considerable differences to idelalisib. Drug Des Devel Ther. 2018 Aug 21;12:2577-2590. doi: 10.2147/DDDT.S142406. eCollection 2018. Review. PubMed PMID: 30174412; PubMed Central PMCID: PMC6109662. 10: Mensah FA, Blaize JP, Bryan LJ. Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date. Onco Targets Ther. 2018 Aug 13;11:4817-4827. doi: 10.2147/OTT.S142264. eCollection 2018. Review. PubMed PMID: 30147333; PubMed Central PMCID: PMC6097514. 11: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500940/ PubMed PMID: 29999999. 12: Dreyling M. A closer look at copanlisib. Clin Adv Hematol Oncol. 2018 Jan;16(1):35-37. PubMed PMID: 29741503. 13: Copanlisib (Aliqopa) for relapsed follicular lymphoma. Med Lett Drugs Ther. 2018 Apr 23;60(1545):e74-e75. PubMed PMID: 29667951. 14: Kim RD, Alberts SR, Peña C, Genvresse I, Ajavon-Hartmann A, Xia C, Kelly A, Grilley-Olson JE. Phase I dose-escalation study of copanlisib in combination with gemcitabine or cisplatin plus gemcitabine in patients with advanced cancer. Br J Cancer. 2018 Feb 20;118(4):462-470. doi: 10.1038/bjc.2017.428. Epub 2018 Jan 18. PubMed PMID: 29348486; PubMed Central PMCID: PMC5830590. 15: Markham A. Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. Review. PubMed PMID: 29127587. 16: Copanlisib Produces Prolonged Responses in Lymphoma. Cancer Discov. 2017 Dec;7(12):OF2. doi: 10.1158/2159-8290.CD-NB2017-147. Epub 2017 Oct 25. PubMed PMID: 29070613. 17: Das M. Copanlisib in heavily pretreated indolent lymphoma. Lancet Oncol. 2017 Nov;18(11):e650. doi: 10.1016/S1470-2045(17)30783-0. Epub 2017 Oct 13. PubMed PMID: 29033198. 18: Dreyling M, Santoro A, Mollica L, Leppä S, Follows GA, Lenz G, Kim WS, Nagler A, Panayiotidis P, Demeter J, Özcan M, Kosinova M, Bouabdallah K, Morschhauser F, Stevens DA, Trevarthen D, Giurescu M, Cupit L, Liu L, Köchert K, Seidel H, Peña C, Yin S, Hiemeyer F, Garcia-Vargas J, Childs BH, Zinzani PL. Phosphatidylinositol 3-Kinase Inhibition by Copanlisib in Relapsed or Refractory Indolent Lymphoma. J Clin Oncol. 2017 Dec 10;35(35):3898-3905. doi: 10.1200/JCO.2017.75.4648. Epub 2017 Oct 4. Erratum in: J Clin Oncol. 2018 Feb 10;36(5):521. PubMed PMID: 28976790. 19: Gerisch M, Schwarz T, Lang D, Rohde G, Reif S, Genvresse I, Reschke S, van der Mey D, Granvil C. Pharmacokinetics of intravenous pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor [(14)C]copanlisib (BAY 80-6946) in a mass balance study in healthy male volunteers. Cancer Chemother Pharmacol. 2017 Sep;80(3):535-544. doi: 10.1007/s00280-017-3383-9. Epub 2017 Jul 11. PubMed PMID: 28714036; PubMed Central PMCID: PMC5573760. 20: Dreyling M, Morschhauser F, Bouabdallah K, Bron D, Cunningham D, Assouline SE, Verhoef G, Linton K, Thieblemont C, Vitolo U, Hiemeyer F, Giurescu M, Garcia-Vargas J, Gorbatchevsky I, Liu L, Koechert K, Peña C, Neves M, Childs BH, Zinzani PL. Phase II study of copanlisib, a PI3K inhibitor, in relapsed or refractory, indolent or aggressive lymphoma. Ann Oncol. 2017 Sep 1;28(9):2169-2178. doi: 10.1093/annonc/mdx289. PubMed PMID: 28633365; PubMed Central PMCID: PMC5834070.