SAR405 |
رقم الكتالوجGC11471
One-Click Copy Product Info
|
SAR405 هو مثبط لـ Vps34 (IC50 = 1.2 نانومول)، يعمل SAR405 على منع الأوتوفاج من التثبيط بواسطة تثبيط mTOR.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1523406-39-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
SAR405 is a highly selective, ATP-competitive class III phosphoinositide 3-kinase (PIK3C3/Vps34) inhibitor with an IC50 value of 1.2nM[1]. PIK3C3 is responsible for catalyzing the production of phosphatidylinositol 3-phosphate (PI(3)P) and serves as a core regulator of intracellular membrane trafficking, autophagy initiation, and endosomal function[2]. SAR405 is frequently employed in research areas including tumor cell proliferation, autophagy regulation, and combination therapies (e.g., synergistic anticancer effects with mTOR inhibitors)[3,4].
In vitro, SAR405 (0.1-50μM) treatment of human pleural mesothelioma H28, H2452, and 211H cell lines for 72h resulted in a concentration-dependent reduction in cell viability, with IC50 values of 10.8μM, 17.4μM, and 12.4μM, respectively[5]. Pretreatment of serum-starved H4IIEC3 cells with SAR405 (1μM) for 2h, followed by stimulation with 100nM insulin for 0, 5, 15, and 30min, significantly inhibited the formation of insulin-induced actin domains[6].
In vivo, aged (16-month-old) C57BL/6 mice treated with SAR405 (5mg/kg/day; i.p.) for 1 month exhibited significantly enhanced succinate dehydrogenase (SDH) staining intensity in tibialis anterior muscle fibers, indicating improved mitochondrial function in aged mouse muscle[7].
References:
[1] Yu X, Long Y C, Shen H M. Differential regulatory functions of three classes of phosphatidylinositol and phosphoinositide 3-kinases in autophagy[J]. Autophagy, 2015, 11(10): 1711-1728.
[2] Zhou X, Wang L, Hasegawa H, et al. Deletion of PIK3C3/Vps34 in sensory neurons causes rapid neurodegeneration by disrupting the endosomal but not the autophagic pathway[J]. Proceedings of the National Academy of Sciences, 2010, 107(20): 9424-9429.
[3] Pasquier B. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells[J]. Autophagy, 2015, 11(4): 725-726.
[4] Ronan B, Flamand O, Vescovi L, et al. A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy[J]. Nature chemical biology, 2014, 10(12): 1013-1019.
[5] Kuwabara Y, Sakai K, Shiraishi K, et al. Effects of Autophagy Inhibition by SAR405, a Selective VPS34 Inhibitor, on Pleural Mesothelioma Cells[J]. Thoracic Cancer, 2026, 17(5): e70255.
[6] Kano F, Murata M. Phosphatidylinositol-3-phosphate-mediated actin domain formation linked to DNA synthesis upon insulin treatment in rat hepatoma-derived H4IIEC3 cells[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2019, 1866(5): 793-805.
[7] Hu Z, Luo Y, Liu Y, et al. Partial inhibition of class III PI3K VPS-34 ameliorates motor aging and prolongs health span[J]. PLoS Biology, 2023, 21(7): e3002165.
| Cell experiment [1]: | |
|
Cell lines |
H28, H2452, and 211H cell lines |
|
Preparation Method |
Human pleural mesothelioma cell lines H28, H2452, and 211H were seeded in 96-well plates and treated with SAR405 (0.1-50μM) for 72h. Cell viability was then assessed using the Cell Counting Kit-8 assay by measuring WST-8 reduction at 450nm. |
|
Reaction Conditions |
0.1-50μM; 72h |
|
Applications |
SAR405 reduces the viability of H28, H2452, and 211H cells in a concentration-dependent manner, with IC50 values of 10.8μM, 17.4μM, and 12.4μM, respectively. |
| Animal experiment [2]: | |
|
Animal models |
Aged (16 months) C57BL/6 mice |
|
Preparation Method |
Aged (16 months) C57BL/6 mice were treated with SAR405 (5mg/kg/day; i.p.) for 1 month, then the tibialis anterior muscles were harvested and stained for SDH activity to assess mitochondrial function in muscle fibers. |
|
Dosage form |
5mg/kg/day; 1 month; i.p. |
|
Applications |
Treatment with SAR405 significantly enhanced the SDH staining intensity of the muscle fibers in the tibialis anterior muscle and improved mitochondrial function in the muscles of aged mice. |
References: [1] Kuwabara Y, Sakai K, Shiraishi K, et al. Effects of Autophagy Inhibition by SAR405, a Selective VPS34 Inhibitor, on Pleural Mesothelioma Cells[J]. Thoracic Cancer, 2026, 17(5): e70255. [2] Hu Z, Luo Y, Liu Y, et al. Partial inhibition of class III PI3K VPS-34 ameliorates motor aging and prolongs health span[J]. PLoS Biology, 2023, 21(7): e3002165. | |
| Cas No. | 1523406-39-4 | SDF | |
| Chemical Name | (S)-1-((5-chloropyridin-3-yl)methyl)-8-((R)-3-methylmorpholino)-2-(trifluoromethyl)-3,4-dihydro-1H-pyrimido[1,2-a]pyrimidin-6(2H)-one | ||
| Canonical SMILES | C[C@H]1N(C(N=C2N3CC[C@@H](C(F)(F)F)N2CC4=CN=CC(Cl)=C4)=CC3=O)CCOC1 | ||
| Formula | C19H21ClF3N5O2 | M.Wt | 443.85 |
| الذوبان | ≥ 22.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.253 mL | 11.2651 mL | 22.5301 mL |
| 5 mM | 450.6 μL | 2.253 mL | 4.506 mL |
| 10 mM | 225.3 μL | 1.1265 mL | 2.253 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)