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SAR405

Chemical Structure : SAR405

CAS No.: 1523406-39-4

SAR405 (SAR-405;SAR 405)

Catalog No.: PC-43055Not For Human Use, Lab Use Only.

SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM.
SAR405 displays no activity against class I and II PI3K isoforms (IC50>10 uM), as well as PIKKs, ATM, ATR and DNA-PK, SMG1.
SAR405 affects both late endosome-lysosome compartments and prevents autophagy, shows synergistic antiproliferative activity in renal tumor cell lines combined with mTOR inhibitor everolimus.
SAR405 enhances the antitumor efficacy of cisplatin in mouse xenograft model of HNSCC.

Physicochemical Properties

M.Wt 443.8506
Formula C19H21ClF3N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 27 mg/mL

Chemical Name/SMILES

4H-Pyrimido[1,2-a]pyrimidin-4-one, 9-[(5-chloro-3-pyridinyl)methyl]-6,7,8,9-tetrahydro-2-[(3R)-3-methyl-4-morpholinyl]-8-(trifluoromethyl)-, (8S)-

References

1. Ronan B, et al. Nat Chem Biol. 2014 Dec;10(12):1013-9.

2. Pasquier B. Autophagy. 2015 Apr 3;11(4):725-6.

3. Valet C, et al. Blood. 2017 Nov 2;130(18):2032-2042.

4. New J, et al. Cancer Res. 2017 Dec 1;77(23):6679-6691.

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