[CAS NO. 1523406-39-4] SAR405
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PRODUCTS SPECIFICATIONS [1523406-39-4]
Store
Catalog
SLK-S7682
Brand
Selleck
CAS
1523406-39-4
DESCRIPTION [1523406-39-4]
Overview
| MDL | MFCD28411361 |
|---|---|
| Molecular Weight | 443.85 |
| Molecular Formula | C19H21ClF3N5O2 |
| SMILES | O=C1C=C(N2[C@H](C)COCC2)N=C3N(CC4=CC(Cl)=CN=C4)[C@H](C(F)(F)F)CCN31 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2530 mL | 11.2651 mL | 22.5301 mL |
| 5 mM | 0.4506 mL | 2.2530 mL | 4.5060 mL |
| 10 mM | 0.2253 mL | 1.1265 mL | 2.2530 mL |
| 50 mM | 0.0451 mL | 0.2253 mL | 0.4506 mL |
Description
SAR405 is a low-molecular-mass kinase inhibitor of (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Targets
| Vps34 [1] |
| 1.2 nM |
In vitro
SAR405 is an inhibitor that was highly specific for Vps34 with regard to protein kinases and other phosphoinositide kinases. SAR405 has an IC50 of 1 nM in the phosphorylation of a PtdIns substrate by human recombinant Vps34 enzyme. This compound shows a binding equilibrium constant KD of 1.52 ± 0.77 nM (± s.d.) and a dissociation rate constant, k, of 3.03 ± 0.55 10/s, corresponding to a residence half-life, t, of 3.8 min. SAR405 does not affect the Akt phosphorylation at concentrations up to 10 μM in the PC3 cell line. SAR405 affects vesicle trafficking from late endosomes to lysosomes. It is also a potent autophagy inhibitor.
References
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