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RO4929097 (RG-4733) γ-Secretase inhibitor

Cat.No.S1575

RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.

RO4929097 (RG-4733) Secretase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 469.4

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Quality Control

Batch: Purity: 99.77%

99.77

Related Targets	HDAC Caspase Proteasome MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP Serine Protease
Other Secretase Inhibitors	DAPT LY411575 Nirogacestat (PF-03084014) Dibenzazepine (YO-01027) MK-0752 Semagacestat (LY450139) Avagacestat (BMS-708163) MDL-28170 L-685,458 Itanapraced (CHF 5074)

Q&A of RO4929097 (RG-4733): Insights Rooted in Extensive Publications, Every Answer Cited

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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 94 mg/mL (200.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 94 mg/mL (200.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 43 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 93 mg/mL (198.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 93 mg/mL (198.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 93 mg/mL (198.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 95%saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.200mg/ml (0.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clear DMSO stock solution to 950 μL of saline and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.700mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 94 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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 ddH₂O, 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.

Read more about RO4929097 (RG-4733) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about RO4929097 (RG-4733) working concentrations for cell culture treatment

RO4929097 (RG-4733) is a potent inhibitor of NOTCH1 (0.46 nM), NOTCH2, NOTCH3, NOTCH4. RO4929097 (RG-4733) exhibits the greatest inhibitory potency toward NOTCH1 (IC50 = 0.46 nM).

Read more about selectivity & specificity

Mechanism of Action

Information	RO4929097 is a potent γ-secretase inhibitor. It affects Notch signaling by blocking cleavage, inhibiting EMT and tumor growth.
Read more about RO4929097 (RG-4733) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about RO4929097 (RG-4733) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	469.4	Formula	C₂₂H₂₀F₅N₃O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	847925-91-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RG-4733			Smiles	CC(C)(C(=O)NCC(C(F)(F)F)(F)F)C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3NC1=O

Read more about storage & stability

Read more comparative analysis about RO4929097 (RG-4733)

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
How about its half-life?

Answer:
Its half-life is about 20 hours based on the following paper: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3869895/

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

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