Shopping Cart

Your shopping cart is currently empty

RLY-2608

Name: RLY-2608
Brand: TargetMol
SKU: T81264
Price: 132 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: Zovegalisib, RLY2608, RLY 2608) Copy Product Info

😃Good

Hot

Synonyms: Zovegalisib, RLY2608, RLY 2608

Catalog No. T81264 Copy Product Info

Purity: 99.87%

😃Good

Hot

RLY-2608 is a small molecule inhibitor, a selective allosteric PI3Kα inhibitor with high selectivity for PIK3CA mutations. This compound effectively inhibits tumor growth in PIK3CA-mutant xenograft models and is primarily used for research on PIK3CA-driven cancers.

Cas No. 2733573-94-7

Pack Size	Price	USA Stock	Global Stock
1 mg	$132	In Stock	In Stock
5 mg	$328	In Stock	In Stock
10 mg	$538	In Stock	In Stock
25 mg	$993	In Stock	In Stock
50 mg	$1,330	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$443	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

Add to Cart

Add to Quotation

Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

Questions

Batch Information

Select Batch

Purity:99.87%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	RLY-2608 is a small molecule inhibitor, a selective allosteric PI3Kα inhibitor with high selectivity for PIK3CA mutations. This compound effectively inhibits tumor growth in PIK3CA-mutant xenograft models and is primarily used for research on PIK3CA-driven cancers.
Targets & IC50	PI3Kα:4 nM
In vitro	Methods: In MCF10A engineered cell lines expressing PI3Kα H1047R or E545K mutations and cancer cells such as T47D and MCF7, cells were treated with gradient concentrations of RLY-2608 for 2 hours (to detect pAKT) or 120 hours (to detect proliferation), using HTRF and CellTiter-Glo assay. Results: RLY-2608 selectively inhibited pAKT and proliferation in mutant cells, while showing weak inhibitory effects on WT PI3Kα-dependent SKBR3 cells.[1]
In vivo	Methods: In T47D (H1047R) and MCF7 (E545K) cell xenografts and ST1056, ST986 PDX models, after tumors reached 200 mm³, RLY-2608 was orally administered (100 mg/kg, twice daily) alone or in combination with fulvestrant or ribociclib. Results: RLY-2608 significantly inhibited tumor growth, with partial regression observed, and insulin levels showed no significant increase compared to the control group.[1]
Synonyms	Zovegalisib, RLY2608, RLY 2608

Chemical Properties

Molecular Weight	608.91
Formula	C₂₉H₁₄ClF₅N₆O₂
Cas No.	2733573-94-7
Smiles	N(C(=O)C1=CC(C(F)(F)F)=CC(F)=C1)C2=C3[C@@H](NC(=O)C3=CC(=C2)C4=C(C#N)N5C(C=C4)=NC=N5)C6=C(Cl)C=CC(F)=C6

Storage & Solubility Information

Storage

Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (131.38 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (8.21 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6423 mL	8.2114 mL	16.4228 mL	82.1139 mL
5 mM	0.3285 mL	1.6423 mL	3.2846 mL	16.4228 mL
10 mM	0.1642 mL	0.8211 mL	1.6423 mL	8.2114 mL
20 mM	0.0821 mL	0.4106 mL	0.8211 mL	4.1057 mL
50 mM	0.0328 mL	0.1642 mL	0.3285 mL	1.6423 mL
100 mM	0.0164 mL	0.0821 mL	0.1642 mL	0.8211 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc