2. PI3K/Akt/mTOR
  3. PI3K
  4. RLY-2608

RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin.

For research use only. We do not sell to patients.

RLY-2608 Chemical Structure

RLY-2608 Chemical Structure

CAS No. : 2733573-94-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1741 In-stock
Solution
10 mM * 1 mL in DMSO USD 1741 In-stock
Solid
1 mg USD 650 In-stock
5 mg USD 1300 In-stock
10 mg USD 2100 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

RLY-2608 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin[1][2][3].

In Vitro

RLY-2608 (1 nM-100 μM, 5 days) inhibits the proliferation and phosphorylated AKT (pAKT) in PIK3CA mutant cancer cell lines independent of the hotspot mutation[2].

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

RLY-2608 Related Antibodies
In Vivo

RLY-2608 (25-100 mg/kg, p.o., twice a day for 50 days) inhibits tumors in tumor xenograft mice models with reduced impact on insulin levels[1].
RLY-2608 (12.5-100 mg/kg, p.o., a single dose for 4 days) demonstrates potent tumor growth inhibition in Balb/c nude female mice bearing HSC-2 tumors[2].

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

Animal Model: Tumor xenograft mice models[1]
Dosage: 25-100 mg/kg
Administration: p.o., twice a day for 50 days
Result: Potentiated tumor regression in tumor xenograft mice models.
Molecular Weight

608.91

Formula

C29H14ClF5N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N[C@@H](C2=CC(F)=CC=C2Cl)C(C1=C3)=C(NC(C4=CC(F)=CC(C(F)(F)F)=C4)=O)C=C3C5=C(C#N)N6C(C=C5)=NC=N6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (164.23 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6423 mL 8.2114 mL 16.4228 mL
5 mM 0.3285 mL 1.6423 mL 3.2846 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 5 mg/mL (8.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
Purity & Documentation

Purity: 99.20%

SDS (251 KB)

COA (260 KB) HNMR (305 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6423 mL 8.2114 mL 16.4228 mL 41.0570 mL
5 mM 0.3285 mL 1.6423 mL 3.2846 mL 8.2114 mL
10 mM 0.1642 mL 0.8211 mL 1.6423 mL 4.1057 mL
15 mM 0.1095 mL 0.5474 mL 1.0949 mL 2.7371 mL
20 mM 0.0821 mL 0.4106 mL 0.8211 mL 2.0528 mL
25 mM 0.0657 mL 0.3285 mL 0.6569 mL 1.6423 mL
30 mM 0.0547 mL 0.2737 mL 0.5474 mL 1.3686 mL
40 mM 0.0411 mL 0.2053 mL 0.4106 mL 1.0264 mL
50 mM 0.0328 mL 0.1642 mL 0.3285 mL 0.8211 mL
60 mM 0.0274 mL 0.1369 mL 0.2737 mL 0.6843 mL
80 mM 0.0205 mL 0.1026 mL 0.2053 mL 0.5132 mL
100 mM 0.0164 mL 0.0821 mL 0.1642 mL 0.4106 mL
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RLY-2608 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:

RLY-26082733573-94-7RLY2608RLY 2608PI3KPhosphoinositide 3-kinaseanti-tumorhyperinsulinemiaPI3K,Inhibitorinhibitorinhibit

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