2. PROTAC Protein Tyrosine Kinase/RTK
  3. Btk PROTACs
  4. L18I

L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964)[1].

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

L18I Chemical Structure

L18I Chemical Structure

CAS No. : 2451070-32-7

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Based on 1 publication(s) in Google Scholar

L18I Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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  • Purity & Documentation

  • References

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Description

L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964)[1].

IC50 & Target

Btk[1]
Molecular Weight

897.98

Formula

C47H51N11O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC=CC(CCCOCCOCCOCCN3C=C(C(N4CCC[C@@H](N5N=C(C6=CC=C(OC7=CC=CC=C7)C=C6)C8=C5N=CN=C8N)C4)=O)N=N3)=C2CN1C9C(NC(CC9)=O)=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 (111.36 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 1.1136 mL 5.5681 mL 11.1361 mL
5 mM 0.2227 mL 1.1136 mL 2.2272 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 (2.78 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.78 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.
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 1.1136 mL 5.5681 mL 11.1361 mL 27.8403 mL
5 mM 0.2227 mL 1.1136 mL 2.2272 mL 5.5681 mL
10 mM 0.1114 mL 0.5568 mL 1.1136 mL 2.7840 mL
15 mM 0.0742 mL 0.3712 mL 0.7424 mL 1.8560 mL
20 mM 0.0557 mL 0.2784 mL 0.5568 mL 1.3920 mL
25 mM 0.0445 mL 0.2227 mL 0.4454 mL 1.1136 mL
30 mM 0.0371 mL 0.1856 mL 0.3712 mL 0.9280 mL
40 mM 0.0278 mL 0.1392 mL 0.2784 mL 0.6960 mL
50 mM 0.0223 mL 0.1114 mL 0.2227 mL 0.5568 mL
60 mM 0.0186 mL 0.0928 mL 0.1856 mL 0.4640 mL
80 mM 0.0139 mL 0.0696 mL 0.1392 mL 0.3480 mL
100 mM 0.0111 mL 0.0557 mL 0.1114 mL 0.2784 mL
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L18I 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:

L18I2451070-32-7BtkPROTACsBruton tyrosine kinaseInhibitorinhibitorinhibit

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