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BAY 80-6946 CAS: 1032568-63-0

Category: Inhibitors
Product Name: BAY 80-6946
Cat No: I000193
CAS No: 1032568-63-0
Synonyms: 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
Molecular Formula: C23H28N8O4
Molecular Weight: 480.5
SMILES: O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN52
InChI: 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)
InChIKey: PZBCKZWLPGJMAO-UHFFFAOYSA-N
Solubility: 10 mM in DMSO
Target: PI3K
IC50: 0.469/3.72 nM(PI3Kα/β) [1]
Storage: powder
CAS 1032568-63-0,BAY 80-6946
  • Description

BAY 80-6946(Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.
IC50 value: 0.469/3.72 nM(PI3Kα/β) [1]
Target: PI3Kα/β
in vitro: BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. BAY 86-9766 inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines [2].
in vivo: BAY 80-6946 is generally well tolerated through the MTD (maximum tolerated dose) of 0.8 mg/kg. PK (pharmacokinetics) 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 [1].

  • Spec

Appearance:white solid powder
Purity: > 98%

  • References


1:First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas. Patnaik A, Appleman LJ, Tolcher AW, Papadopoulos KP, Beeram M, Rasco DW, Weiss GJ, Sachdev JC, Chadha M, Fulk M, Ejadi S, Mountz JM, Lotze MT, Toledo FG, Chu E, Jeffers M, Peña C, Xia C, Reif S, Genvresse I, Ramanathan RK.Ann Oncol. 2016 Oct;27(10):1928-40. doi: 10.1093/annonc/mdw282. PMID: 27672108 Free PMC Article
2:Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946). Scott WJ, Hentemann MF, Rowley RB, Bull CO, Jenkins S, Bullion AM, Johnson J, Redman A, Robbins AH, Esler W, Fracasso RP, Garrison T, Hamilton M, Michels M, Wood JE, Wilkie DP, Xiao H, Levy J, Stasik E, Liu N, Schaefer M, Brands M, Lefranc J.ChemMedChem. 2016 Jul 19;11(14):1517-30. doi: 10.1002/cmdc.201600148. Epub 2016 Jun 16. PMID: 27310202 Free PMC Article
3:A preclinical evaluation of the PI3K alpha/delta dominant inhibitor BAY 80-6946 in HER2-positive breast cancer models with acquired resistance to the HER2-targeted therapies trastuzumab and lapatinib. Elster N, Cremona M, Morgan C, Toomey S, Carr A, O'Grady A, Hennessy BT, Eustace AJ.Breast Cancer Res Treat. 2015 Jan;149(2):373-83. doi: 10.1007/s10549-014-3239-5. Epub 2014 Dec 21. PMID: 25528022
4:The novel PI3 kinase inhibitor, BAY 80-6946, impairs melanoma growth in vivo and in vitro. Schneider P, Schön M, Pletz N, Seitz CS, Liu N, Ziegelbauer K, Zachmann K, Emmert S, Schön MP.Exp Dermatol. 2014 Aug;23(8):579-84. doi: 10.1111/exd.12470. PMID: 24942196
5:Preliminary results of a phase II study of single agent Bay 80-6946, a Novel PI3K inhibitor, in patients with relapsed/refractory, indolent or aggressive lymphoma. [No authors listed]Clin Adv Hematol Oncol. 2014 Feb;12(2 Suppl 5):14-6. No abstract available. PMID: 24852792
6:BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Liu N, Rowley BR, Bull CO, Schneider C, Haegebarth A, Schatz CA, Fracasso PR, Wilkie DP, Hentemann M, Wilhelm SM, Scott WJ, Mumberg D, Ziegelbauer K.Mol Cancer Ther. 2013 Nov;12(11):2319-30. doi: 10.1158/1535-7163.MCT-12-0993-T. Epub 2013 Oct 29. PMID: 24170767 Free Article


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