[CAS NO. 2365241-79-6] PI4KIIIbeta-IN-11
PRODUCTS SPECIFICATIONS [2365241-79-6]
DESCRIPTION [2365241-79-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 581.71 |
| Molecular Formula | C33H39N7O3 |
| SMILES | CN1C(C2=CC=CC(CNC3=CC(C(C)(O)C)=NC4=C(C5=CC(C(N(C)[C@@H](C)CO)=O)=C(C=C5)C)C(C)=NN34)=C2)=NC=C1 |
Summary
PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ , with a mean pIC 50 value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum [1] [2] .
IC50 & Target
|
PI4KIIIβ 9.1 (pIC 50 ) |
In Vitro
PI4KIIIβ may be a relevant target protein for inhibition of Hedgehog signaling, and regulates trafficking from the Golgi system to the plasma membrane
[1]
.
PI4KIIIbeta-IN-11 (compound 22) (0.5 μM; 0-45 min) shows metabolic stability in human microsomes, with the intrinsic clearance of 33.7 mL/min/g
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PI4KIIIbeta-IN-11 (compound 22) (1 mg/kg; i.v.; last over 1 h) displays a low spleen concentration in rats
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Wistar Han Rats [2] |
| Dosage: | 1 mg/kg |
| Administration: | Intravenous injection, formulated in 2% DMSO in Kleptose (aq, 10% w/v); over 1 hour; euthanised at 12 h |
| Result: | Showed a low concentration in spleen of 5.54 ng/g. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [1] Kremer L, et al. Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß. Angew Chem Int Ed Engl. 2019 Nov 11;58(46):16617-16628.
- [2] Barton Nicholas Paul, et al. Preparation of pyrazolopyrimidinamines derivatives as PI4kIII-beta inhibitors: World Intellectual Property Organization, WO2019141694. 2019-07-25.