SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

Product information

CAS Number: 1523406-39-4

Molecular Weight: 443.85

Formula: C19H21ClF3N5O2

Chemical Name: (2S)-1-[(5-chloropyridin-3-yl)methyl]-8-[(3R)-3-methylmorpholin-4-yl]-2-(trifluoromethyl)-1H,2H,3H,4H,6H-pyrimido[1,2-a][1,3]diazin-6-one

Smiles: C[C@@H]1COCCN1C1=CC(=O)N2CC[C@H](N(CC3=CN=CC(Cl)=C3)C2=N1)C(F)(F)F

InChiKey: SPDQRCUBFSRAFI-DOMZBBRYSA-N

InChi: InChI=1S/C19H21ClF3N5O2/c1-12-11-30-5-4-26(12)16-7-17(29)27-3-2-15(19(21,22)23)28(18(27)25-16)10-13-6-14(20)9-24-8-13/h6-9,12,15H,2-5,10-11H2,1H3/t12-,15+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 27 mg/mL (60.83 mM). H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line. SAR405 prevents autophagy and synergizes with mTOR inhibition in tumor cells. SAR405 prevents autophagosome formation with an IC50 of 42 nM. Treatment of starved cells with SAR405 completely inhibits the conversion to LC3-II in a dose-dependent manner. The effect of SAR405 on autophagy is then investigated. The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC50=419 nM). The conversion of LC3-I into LC3-II is also analyzed by western blotting on wild-type HeLa and H1299 cells.

Products are for research use only. Not for human use.