2. PI3K/Akt/mTOR
  3. PI3K
  4. HL-8

HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases.

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

HL-8 Chemical Structure

HL-8 Chemical Structure

CAS No. : 2766352-64-9

Size Price Stock Quantity
1 mg USD 676 In-stock
5 mg USD 1420 In-stock
10 mg USD 2340 In-stock
25 mg USD 4680 In-stock
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases[1].

Molecular Weight

1144.27

Formula

C57H59F2N11O9S2
CAS No.
Unlabeled CAS

Appearance

Solid

Color

White to off-white

SMILES

COC1=NC=C(C=C1NS(=O)(C2=C(C=C(C=C2)F)F)=O)C3=CN4C(C5=NN=C(O5)C6=C(C=CC=C6)C(NCCCCCCC(N[C@@H](C(C)(C)C)C(N7C[C@H](C[C@@H]7C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)O)=O)=O)=O)=CN=C4C=C3
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 (87.39 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 0.8739 mL 4.3696 mL 8.7392 mL
5 mM 0.1748 mL 0.8739 mL 1.7478 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 (2.18 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 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
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 0.8739 mL 4.3696 mL 8.7392 mL 21.8480 mL
5 mM 0.1748 mL 0.8739 mL 1.7478 mL 4.3696 mL
10 mM 0.0874 mL 0.4370 mL 0.8739 mL 2.1848 mL
15 mM 0.0583 mL 0.2913 mL 0.5826 mL 1.4565 mL
20 mM 0.0437 mL 0.2185 mL 0.4370 mL 1.0924 mL
25 mM 0.0350 mL 0.1748 mL 0.3496 mL 0.8739 mL
30 mM 0.0291 mL 0.1457 mL 0.2913 mL 0.7283 mL
40 mM 0.0218 mL 0.1092 mL 0.2185 mL 0.5462 mL
50 mM 0.0175 mL 0.0874 mL 0.1748 mL 0.4370 mL
60 mM 0.0146 mL 0.0728 mL 0.1457 mL 0.3641 mL
80 mM 0.0109 mL 0.0546 mL 0.1092 mL 0.2731 mL
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HL-8 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:

HL-82766352-64-9HL8HL 8PI3KPhosphoinositide 3-kinasePI3K kinasecancer diseasesInhibitorinhibitorinhibit

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