2. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR
  3. Ras PI3K Akt
  4. VVD-699

VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer.

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

VVD-699

VVD-699 Chemical Structure

CAS No. : 3055319-82-6

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 Customer Validation

VVD-699 Related Antibodies

Top Publications Citing Use of Products

View All Ras Isoform Specific Products:

View All Isoforms
K-Ras H-Ras N-Ras Ras

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer[1].

IC50 & Target[1]

PI3Kα

104 nM (IC50)

In Vitro

VVD-699 (0.002-5 μM; 2 h) inhibits phosphorylated AKT in KRASGly12Ser A549 human lung cancer cells[1].

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

VVD-699 Related Antibodies
In Vivo

Combination treatment with VVD-699 (30 mg/kg; p.o.; twice daily) and Sotorasib (HY-114277) yields greater benefits than the combination of Sotorasib and Binimetinib (HY-15202) in the H2122 xenograft mouse model, and triple combination of the three agents induces durable tumor regression[1].

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

Animal Model: Immunodeficient mice[1]
Dosage: 30 mg/kg; 100 mg/kg
Administration: p.o.; twice daily (BID); 3 days
Result: Induced no significant changes in blood glucose levels or plasma insulin levels with 30 mg/kg or 100 mg/kg dosing.
Achieved near-maximal p110α-C242 target engagement in liver and spleen tissue with both doses.
Molecular Weight

573.10

Formula

C25H30ClFN2O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(C2=C(Cl)C=CC=C2)=C(S(N3CC[C@](C(N[C@@H](/C=C\S(C)(=O)=O)C)=O)(F)C[C@H]3C)(=O)=O)C=C1
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 (174.49 mM; Need ultrasonic; 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 1.7449 mL 8.7245 mL 17.4490 mL
5 mM 0.3490 mL 1.7449 mL 3.4898 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
×
Volume
×
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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.36 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.36 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.

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
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 1.7449 mL 8.7245 mL 17.4490 mL 43.6224 mL
5 mM 0.3490 mL 1.7449 mL 3.4898 mL 8.7245 mL
10 mM 0.1745 mL 0.8724 mL 1.7449 mL 4.3622 mL
15 mM 0.1163 mL 0.5816 mL 1.1633 mL 2.9082 mL
20 mM 0.0872 mL 0.4362 mL 0.8724 mL 2.1811 mL
25 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7449 mL
30 mM 0.0582 mL 0.2908 mL 0.5816 mL 1.4541 mL
40 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0906 mL
50 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8724 mL
60 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7270 mL
80 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5453 mL
100 mM 0.0174 mL 0.0872 mL 0.1745 mL 0.4362 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

VVD-699 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:

VVD-6993055319-82-6VVD699VVD 699RasPI3KAktPhosphoinositide 3-kinasePKBProtein kinase BPI3K/AKT signalingp110αRAS binding domainHER2 over-expressing cancer cellsHEK293T cellsRAS-p110α interactionRAS mutant cancer cellsJurkat cellscysteine 242H358 cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
VVD-699
Cat. No.:
HY-173405
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.