Copanlisib HCl
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MedKoo CAT#: 206945

CAS#: 1402152-13-9 (HCl)

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

Size
Price

25mg
USD 150
200mg
USD 750
2g
USD 4250
Size
Price

50mg
USD 250
500mg
USD 1650
5g
USD 6850
Size
Price

100mg
USD 450
1g
USD 2850

Copanlisib HCl, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 4g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206945
Name: Copanlisib HCl
CAS#: 1402152-13-9 (HCl)
Chemical Formula: C23H30Cl2N8O4
Exact Mass:
Molecular Weight: 553.445
Elemental Analysis: C, 49.92; H, 5.46; Cl, 12.81; N, 20.25; O, 11.56


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

Synonym: Copanlisib HCl; Copanlisib dihydrochloride; BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; Copanlisib; 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 (1:2)

InChi Key: STGQPVQAAFJJFX-UHFFFAOYSA-N

InChi Code: STGQPVQAAFJJFX-UHFFFAOYSA-N

SMILES Code: O=C(C1=CN=C(N)N=C1)NC2=NC3=C(C=CC(OCCCN4CCOCC4)=C3OC)C5=NCCN25.[H]Cl.[H]Cl


Technical Data

Appearance:
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

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


References

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.