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BAY 80-6946 (Copanlisib)PI3K inhibitor

BAY 80-6946 (Copanlisib)

Catalog No. B2178
Size Price Stock Qty
5mg $190.00 In stock
10mg $260.00 In stock
50mg $618.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BAY 80-6946 (Copanlisib)

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Chemical Properties

Cas No. 1032568-63-0 SDF Download SDF
Chemical Name 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
Canonical SMILES COC1=C(C=CC2=C1N=C(N3C2=NCC3)NC(=O)C4=CN=C(N=C4)N)OCCCN5CCOCC5
Formula C23H28N8O4 M.Wt 480.52
Solubility Limited solubility Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Several phosphatidylinositol-3-kinase (PI3K) inhibitors are being investigated as a treatment for patients with B-cell malignancies. Such agents prevent activation of PI3K enzymes that are hyperactive in many B-cell malignancies and associated with tumor progression. Copanlisib is a novel pan-Class I phosphatidylinositol-3-kinase (PI3K) inhibitor with potent preclinical inhibitory activity against both PI3K-d and PI3K-α isoforms.
In vitro: BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity, which inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines [1].
In vivo: BAY 80-6946 is generally well tolerated through the maximum tolerated dose (MTD) of 0.8 mg/kg. pharmacokinetics (PK) results support dosing weekly. Grade 2 or 3 hyperglycemia in the first 24 hrs after receiving a MTD dose. Pharmacokinetics, clinical SD as well as FDG-PET data are consistent with effective exposure and PI3K pathway inhibition. [2].
Clinical trial: Copanlisib (BAY 80-6946), developed by Bayer, is a selective Class I phosphoinositide 3-kinase inhibitor which has shown promise in Phase I/II clinical trials for the treatment of non-Hodgkin lymphoma and chronic lymphocytic leukemia. Phase II study shows that Copanlisib is active as a single-agent in heavily pretreated, advanced refractory/relapsed FL, MZL, , CLL and SLL. Copanlisib exhibited an acceptable toxicity profile, which was consistent with previous findings (https://ash.confex.com/ash/2014/webprogram/Paper70672.html).
References:
[1] Patnaik A, et al. J Clin Oncol, 29, 2011, (suppl, abstr 3035)
[2] Andrea H, et al. Cancer Res, 2012; 72(8), (suppl, Abstract 869)