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Leniolisib

Cat. No. M10186
Leniolisib Structure
Synonym:

CDZ173

Size Price Availability Quantity
5mg USD 192  USD192 In stock
10mg USD 306  USD306 In stock
25mg USD 586  USD586 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor with IC50 of 11 nM. Leniolisib has IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Leniolisib inhibits a large spectrum of immune cell functions, as demonstrated in B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells.

In vivo, Leniolisib (CDZ173) inhibits B cell activation in rats and monkeys in a concentration- and time-dependent manner. After prophylactic or therapeutic dosing, Leniolisib potently inhibited antigen-specific antibody production and reduced disease symptoms in a rat collagen-induced arthritis model. Oral Leniolisib led to a dose-dependent reduction in PI3K/AKT pathway activity assessed ex vivo and improved immune dysregulation.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 450.46
Formula C21H25F3N6O2
CAS Number 1354690-24-6
Purity >99%
Solubility DMSO 86 mg/mL
Storage at -20°C
References

[1] David Pearson, et al. Xenobiotica. 19 F-NMR-based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers

[2] Stefan De Buck, et al. Biopharm Drug Dispos. CYP3A but not P-gp plays a relevant role in the in vivo intestinal and hepatic clearance of the delta-specific phosphoinositide-3 kinase inhibitor leniolisib

[3] V Koneti Rao, et al. Blood. Effective activated PI3Kδ syndrome-targeted therapy with the PI3Kδ inhibitor leniolisib

[4] Klemens Hoegenauer, et al. ACS Med Chem Lett. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Leniolisib, CDZ173 supplier, PI3K, inhibitors

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