2. PI3K/Akt/mTOR
  3. PI3K
  4. Vulolisib

Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity.

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

Vulolisib Chemical Structure

Vulolisib Chemical Structure

CAS No. : 2390105-79-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 727 In-stock
Solution
10 mM * 1 mL in DMSO USD 727 In-stock
Solid
1 mg USD 310 In-stock
5 mg USD 780 In-stock
10 mg USD 1250 In-stock
25 mg USD 2500 In-stock
50 mg USD 4050 In-stock
100 mg USD 6500 In-stock
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Based on 1 publication(s) in Google Scholar

Vulolisib Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity[1].

IC50 & Target[1]

PI3Kα

0.2 nM (IC50)

PI3Kβ

168 nM (IC50)

PI3Kγ

90 nM (IC50)

PI3Kδ

49 nM (IC50)

In Vitro

Vulolisib has antiproliferative activity against PI3Kα-mutant cell lines HCC1954 (H1047R), HGC-27 (E542K) and MKN1 (E545K) with IC50s of 21 nM, 60 nM and 40 nM, respectively[1].

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

Vulolisib Related Antibodies
In Vivo

Vulolisib (10, 30 and 60 mg/kg; IG; daily for 7days) exhibits better tolerance and exposure than Inavolisib[1].
Vulolisib (10mg/kg; PO; daily for 19 days) inhibits tumor growth with TGI of 132%[1].
Vulolisib (5 mg/kg; IG, single dosage) exhibits favorable pharmacokinetic property[1].
Pharmacokinetic Parameters of Vulolisib in male Balb/c mice[1].

IG (5 mg/kg)
tmax (h) 0.5
Cmax (ng/mL) 1057
AUC0-t (ng/mL·h) 2185
AUC0-∞ (ng/mL·h) 2274
t1/2 (h) 1.6
MRT (h) 2.2

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 10, 30 and 60 mg/kg
Administration: IG; daily for 7days
Result: Exhibited better tolerance and exposure than Inavolisib.
Animal Model: Female BALB/c nude mice (6-8 weeks; injected with HCC1954)[1]
Dosage: 10mg/kg
Administration: PO; daily for 19 days
Result: Inhibited tumor growth with TGI of 132%.
Animal Model: Male Balb/c mice[1]
Dosage: 5 mg/kg
Administration: IG, single dosage (Pharmacokinetic Analysis)
Result: Exhibited favorable pharmacokinetic property.
Molecular Weight

423.44

Formula

C18H19F2N5O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC([C@H](C)NC1=CC=C(C2=NC(N3[C@@H](CSC3=O)C(F)F)=CN2CCO4)C4=C1)=O
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 (236.16 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 2.3616 mL 11.8080 mL 23.6161 mL
5 mM 0.4723 mL 2.3616 mL 4.7232 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.90 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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 (5.90 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
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 2.3616 mL 11.8080 mL 23.6161 mL 59.0402 mL
5 mM 0.4723 mL 2.3616 mL 4.7232 mL 11.8080 mL
10 mM 0.2362 mL 1.1808 mL 2.3616 mL 5.9040 mL
15 mM 0.1574 mL 0.7872 mL 1.5744 mL 3.9360 mL
20 mM 0.1181 mL 0.5904 mL 1.1808 mL 2.9520 mL
25 mM 0.0945 mL 0.4723 mL 0.9446 mL 2.3616 mL
30 mM 0.0787 mL 0.3936 mL 0.7872 mL 1.9680 mL
40 mM 0.0590 mL 0.2952 mL 0.5904 mL 1.4760 mL
50 mM 0.0472 mL 0.2362 mL 0.4723 mL 1.1808 mL
60 mM 0.0394 mL 0.1968 mL 0.3936 mL 0.9840 mL
80 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7380 mL
100 mM 0.0236 mL 0.1181 mL 0.2362 mL 0.5904 mL
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Vulolisib 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:

Vulolisib2390105-79-8PI3KPhosphoinositide 3-kinasePI3KαPI3KβPI3KγPI3KδantiproliferativeantineoplasticHCC1954HGC-27MKN1BALB/ctumorInhibitorinhibitorinhibit

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