SAR405

Name: SAR405
Brand: MedChemExpress
SKU: HY-12481
Rating: 5.0 (35 reviews)

Cat. No.: HY-12481 Purity: 99.74%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

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CAS No. : 1523406-39-4

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
2 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 35 publication(s) in Google Scholar

Other Forms of SAR405:

SAR405 R enantiomer In-stock

35 Publications Citing Use of MCE SAR405

In Vivo Efficacy Study

RT-PCR

: SAR405 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2021 Apr;53(4):435-444. [Abstract]; Immunofluorescence staining of LC3B in uninfected or SARS-CoV-2-infected Huh7 cells treated with SAR405 (12.5 μM; 6 h) showed that PI3K type 3 inhibition completely abolished the formation of LC3-positive puncta and induced vacuoles in treated cells.

: SAR405 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2021 Apr;53(4):435-444. [Abstract]; Time series experiments showed an early stage post-receptor binding effect of the PI3K type 3 inhibitor SAR405 on HCoV-229E infection. Huh7 cells were infected, treated with SAR405 at different timepoints, and followed by determination of viral RNA levels at 10 hours post infection by qPCR. Inhibition of HCoV-229E by SAR405 occurred later in the viral life cycle than the attachment stage, as benchmarked by the attachment inhibitor Urtica dioica agglutinin (UDA), but earlier than the onset of intracellular replication as identified using the viral RNA synthesis inhibitor remdesivir.

: SAR405 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2021 Aug;18(8):2024-2039. [Abstract]; PIK3C3 was an important regulator of myeloid cell function and a potential therapeutic target for treating EAE. SAR405 treatment delayed the onset of EAE. EAE was induced by active immunization with MOG35–55 peptide, and SAR405 (10 mg/kg; once daily) was administered orally starting 3 days after immunization for 11 consecutive days.

: SAR405 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Cell Res. 2019 May;1866(5):793-805. [Abstract]; Serum-starved H4IIEC3 cells are treated with 100 nM ins for 0, 5, 15, and 30 min, and electrophoresed protein extracts subjected to western blotting using antibodies against pAktS473 and Akt.

: SAR405 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Cell Res. 2019 May;1866(5):793-805. [Abstract]; Serum-starved H4IIEC3 cells are treated with 100 nM ins for 0, 5, 15, and 30 min and electrophoresed protein extracts subjected to western blotting using antibodies against total or phosphorylated p42/p44 MAPK.

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

Vps34

1.2 nM (IC₅₀)

Vps34

1.5 nM (Kd)

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
Cortical neurone	EC₅₀	2.4 3 Compound: SAR405	Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay	[PMID: 30840447]
Cortical neurone	EC₅₀	2.4 3 Compound: SAR405	Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay	[PMID: 30840447]
Cortical neurone	EC₅₀	2.4 3 Compound: SAR405	Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay	[PMID: 30840447]
HeLa	IC₅₀	27 1 Compound: 69; SAR405	Inhibition of Vps34 in human HeLa cells expressing GFP-FYVE Inhibition of Vps34 in human HeLa cells expressing GFP-FYVE	[PMID: 29211480]

In Vitro

The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line^[1].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

분자량

443.85

화학식

C₁₉H₂₁ClF₃N₅O₂

CAS No.

1523406-39-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N(C2=NC(N3[C@H](C)COCC3)=C1)CC[C@@H](C(F)(F)F)N2CC4=CC(Cl)=CN=C4

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : ≥ 27 mg/mL (60.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.74%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (253 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Ronan B, et al. A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy. Nat Chem Biol. 2014 Dec;10(12):1013-9. [Content Brief]

[2]. Pasquier B. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells. Autophagy. 2015 Apr 3;11(4):725-6. [Content Brief]

Kinase Assay
^[1]

KiNativ profiling is performed. Jurkat cell lysates are treated with 1 μM of SAR405. After 15-min incubation, the desthiobiotin-ATP-acylphosphate probe is added and incubated for 10 min. Samples are prepared for targeted MS analysis. Briefly, samples are prepared for trypsin digestion (denature and then reduce alkylate) and digested with trypsin, and desthiobiotinylated peptides are enriched on streptavidin resin. Enriched probe-labeled peptides are analyzed by LC tandem MS on a Thermo-LTQ ion trap mass spectrometer using proprietary data collection methodology. All quantification is performed by extracting characteristic fragment ion signals from targeted MS/MS spectra and comparing signals in control and treated samples^[1].

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

[1]. Ronan B, et al. A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy. Nat Chem Biol. 2014 Dec;10(12):1013-9. [Content Brief]

[2]. Pasquier B. SAR405, a PIK3C3/Vps34 inhibitor that prevents autophagy and synergizes with MTOR inhibition in tumor cells. Autophagy. 2015 Apr 3;11(4):725-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2530 mL	11.2651 mL	22.5301 mL	56.3253 mL
	5 mM	0.4506 mL	2.2530 mL	4.5060 mL	11.2651 mL
	10 mM	0.2253 mL	1.1265 mL	2.2530 mL	5.6325 mL
	15 mM	0.1502 mL	0.7510 mL	1.5020 mL	3.7550 mL
	20 mM	0.1127 mL	0.5633 mL	1.1265 mL	2.8163 mL
	25 mM	0.0901 mL	0.4506 mL	0.9012 mL	2.2530 mL
	30 mM	0.0751 mL	0.3755 mL	0.7510 mL	1.8775 mL
	40 mM	0.0563 mL	0.2816 mL	0.5633 mL	1.4081 mL
	50 mM	0.0451 mL	0.2253 mL	0.4506 mL	1.1265 mL
	60 mM	0.0376 mL	0.1878 mL	0.3755 mL	0.9388 mL

SAR405 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAR4051523406-39-4SAR 405SAR-405PI3KAutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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SAR405

고객리뷰

Other Forms of SAR405:

SAR405 Related Antibodies

35 Publications Citing Use of MCE SAR405

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

SAR405 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

SAR405 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report