Copanlisib free base

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

MedKoo CAT#: 204570

CAS#: 1032568-63-0 (free base)

Description: Copanlisib also known as BAY 80-6946, is a potent phosphoinositide 3-kinase (PI3K) inhibitor. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Copanlisib was approved for the treatment of adult patients experiencing relapsed follicular lymphoma who have received at least two prior systemic therapies.

Price and Availability


USD 150
USD 750
USD 3950

USD 250
USD 1650
USD 5850

USD 450
USD 2850
USD 9650

Copanlisib free base, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 8g may be 2 weeks.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 204570
Name: Copanlisib free base
CAS#: 1032568-63-0 (free base)
Chemical Formula: C23H28N8O4
Exact Mass: 480.22335
Molecular Weight: 480.52
Elemental Analysis: C, 57.49; H, 5.87; N, 23.32; O, 13.32

Related CAS #: 1402152-13-9 (HCl)   1032568-63-0 (free base)    

Synonym: BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; Copanlisib free base

IUPAC/Chemical Name: 2-amino-N-(7-methoxy-8-(3-morpholinopropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyrimidine-5-carboxamide


InChi Code: InChI=1S/C23H28N8O4/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)


Technical Data

white solid powder

>95% (or refer to the 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).

BAY80-6946 does not have good solubility in common solvents. BAY80-6946 is soluble in 5% HCl, slightly soluble in DMSO, not soluble in water.

Shelf Life:
>2 years if stored properly

Drug Formulation:
Method 1: For in vitro studies, 5 mmol/L stock solution of BAY 80-6946 (in dimethyl sulfoxide with 10 mmol/L trifluoroacetic acid) was used - see Mol Cancer Ther. 2013 Nov;12(11):2319-30.

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

Harmonized System Code:

Additional Information

BAY 80-6946 is a potent and highly selective reversible pan-Class I PI3K inhibitor with anti-tumor activity in a panel of preclinical models.  A phase I dose escalation multicenter study showed that BAY 80-6946 was generally well tolerated through the MTD of 0.8 mg/kg. PK results support weekly dosing. Grade 2/3 hyperglycemia in the first 24 hrs after receiving a dose is common at the MTD. PK, clinical SD and FDG-PET data are consistent with effective exposure and PI3K pathway inhibition. (source: J Clin Oncol 29: 2011 (suppl; abstr 3035)
Tips for making stock solution
Due to its chemical nature, pure BAY80-6946 solid powder was found to have very low solubility in common organic solvents. This has been reported in the literature. User may use the following method as a reference when making stock solution: 2 mg BAY80-6946 is placed in a clear vial. To this vial, 10 µL 10% HCl is added. The vial is capped and shaken for a few seconds to allow HCl solution to wet the crystals of BAY80-6946. Then 90 µL water is added, and shaken for a few second, which will give a clear stock solution at 20 mg /mL. This solution can be further diluted using 0.5% HCl water solution.
This solution can be further diluted using 0.5% HCl water solution.
Pure BAY80-6946 has very low solubility, because of its chemical property, not because of the poor quality of our product. Molecule of BAY80-6946 contains several basic nitrogen atoms, after protonated by HCl, its solubility will be enhanced. For in vitro studies, 5 mmol/L stock solution of BAY 80-6946 (in dimethyl sulfoxide with 10 mmol/L trifluoroacetic acid) was used - see Mol Cancer Ther. 2013 Nov;12(11):2319-30.


1: Milewska M, Cremona M, Morgan C, O'Shea J, Carr A, Velanki SH, Hopkins AM, Toomey S, Madden SF, Hennessy BT, Eustace AJ. Development of a personalized therapeutic strategy for ERBB-gene-mutated cancers. Ther Adv Med Oncol. 2018 Jan 9;10:1758834017746040. doi: 10.1177/1758834017746040. eCollection 2018. PubMed PMID: 29383036; PubMed Central PMCID: PMC5784557.

2: 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.

3: Thieblemont C. Improved biological insight and influence on management in indolent lymphoma. Talk 3: update on nodal and splenic marginal zone lymphoma. Hematology Am Soc Hematol Educ Program. 2017 Dec 8;2017(1):371-378. doi: 10.1182/asheducation-2017.1.371. Review. PubMed PMID: 29222281.

4: Simpson I. An industry update: the latest developments in therapeutic delivery. Ther Deliv. 2018 Jan;9(1):9-15. doi: 10.4155/tde-2017-0109. PubMed PMID: 29216806.

5: Greenwell IB, Ip A, Cohen JB. PI3K Inhibitors: Understanding Toxicity Mechanisms and Management. Oncology (Williston Park). 2017 Nov 15;31(11):821-8. Review. PubMed PMID: 29179250.

6: O'Shea J, Cremona M, Morgan C, Milewska M, Holmes F, Espina V, Liotta L, O'Shaughnessy J, Toomey S, Madden SF, Carr A, Elster N, Hennessy BT, Eustace AJ. A preclinical evaluation of the MEK inhibitor refametinib in HER2-positive breast cancer cell lines including those with acquired resistance to trastuzumab or lapatinib. Oncotarget. 2017 Jul 22;8(49):85120-85135. doi: 10.18632/oncotarget.19461. eCollection 2017 Oct 17. PubMed PMID: 29156708; PubMed Central PMCID: PMC5689598.

7: Markham A. Copanlisib: First Global Approval. Drugs. 2017 Dec;77(18):2057-2062. doi: 10.1007/s40265-017-0838-6. PubMed PMID: 29127587.

8: Argnani L, Broccoli A, Zinzani PL. Cutaneous T-cell lymphomas: Focusing on novel agents in relapsed and refractory disease. Cancer Treat Rev. 2017 Dec;61:61-69. doi: 10.1016/j.ctrv.2017.10.007. Epub 2017 Oct 28. Review. PubMed PMID: 29102679.

9: 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.

10: 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.

11: 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. PubMed PMID: 28976790.

12: Broccoli A, Argnani L, Zinzani PL. Peripheral T-cell lymphomas: Focusing on novel agents in relapsed and refractory disease. Cancer Treat Rev. 2017 Nov;60:120-129. doi: 10.1016/j.ctrv.2017.09.002. Epub 2017 Sep 18. Review. PubMed PMID: 28946015.

13: Lampson BL, Brown JR. PI3Kδ-selective and PI3Kα/δ-combinatorial inhibitors in clinical development for B-cell non-Hodgkin lymphoma. Expert Opin Investig Drugs. 2017 Nov;26(11):1267-1279. doi: 10.1080/13543784.2017.1384815. Epub 2017 Oct 6. Review. PubMed PMID: 28945111; PubMed Central PMCID: PMC5747968.

14: Robak P, Robak T. Novel synthetic drugs currently in clinical development for chronic lymphocytic leukemia. Expert Opin Investig Drugs. 2017 Nov;26(11):1249-1265. doi: 10.1080/13543784.2017.1384814. Epub 2017 Oct 3. Review. PubMed PMID: 28942659.

15: 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.

16: 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.

17: Lim SY, Menzies AM, Rizos H. Mechanisms and strategies to overcome resistance to molecularly targeted therapy for melanoma. Cancer. 2017 Jun 1;123(S11):2118-2129. doi: 10.1002/cncr.30435. Review. PubMed PMID: 28543695.

18: Zinzani PL, Broccoli A. Possible novel agents in marginal zone lymphoma. Best Pract Res Clin Haematol. 2017 Mar - Jun;30(1-2):149-157. doi: 10.1016/j.beha.2016.07.003. Epub 2016 Nov 4. Review. PubMed PMID: 28288710.

19: Paul J, Soujon M, Wengner AM, Zitzmann-Kolbe S, Sturz A, Haike K, Keng Magdalene KH, Tan SH, Lange M, Tan SY, Mumberg D, Lim ST, Ziegelbauer K, Liu N. Simultaneous Inhibition of PI3Kδ and PI3Kα Induces ABC-DLBCL Regression by Blocking BCR-Dependent and -Independent Activation of NF-κB and AKT. Cancer Cell. 2017 Jan 9;31(1):64-78. doi: 10.1016/j.ccell.2016.12.003. PubMed PMID: 28073005.

20: Doi T, Fuse N, Yoshino T, Kojima T, Bando H, Miyamoto H, Kaneko M, Osada M, Ohtsu A. A Phase I study of intravenous PI3K inhibitor copanlisib in Japanese patients with advanced or refractory solid tumors. Cancer Chemother Pharmacol. 2017 Jan;79(1):89-98. doi: 10.1007/s00280-016-3198-0. Epub 2016 Dec 3. PubMed PMID: 27915408; PubMed Central PMCID: PMC5225172.