2. PROTAC Autophagy Apoptosis
  3. E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis
  4. Thalidomide-NH-C6-NH-Boc

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).

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Thalidomide-NH-C6-NH-Boc Chemical Structure

Thalidomide-NH-C6-NH-Boc Chemical Structure

CAS No. : 2093536-13-9

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Based on 1 publication(s) in Google Scholar

Thalidomide-NH-C6-NH-Boc Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) MDM2 Cereblon cIAP1 Aryl Hydrocarbon Receptor TRIM21

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A)[1].
IC50 & Target[1]

Cereblon

 

In Vitro

MI-389 (0-1 μM; 72 hours) decreases cell growth with an EC50 value of 21.3 nM, which is comparable to the cellular potency of sunitinib (EC50=17.3 nM)[1].
MI-389 (0-500 nM; 72 hours) leads to GSPT1 destabilization fastly as a dosepdependent manner. It shows a complete GSPT1 depletion at 100 nM[1].

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

Thalidomide-NH-C6-NH-Boc Related Antibodies

Cell Viability Assay[1]

Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1
Concentration: 0-1 μM
Incubation Time: 72 hours
Result: Outperform decreased-antiproliferative effect than sunitinib

Western Blot Analysis[1]

Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1
Concentration: 1 nM, 5 nM, 10 nM, 50 nM, 100 nM, 500 nM
Incubation Time: 4 hours
Result: Decreased GSPT-1 protein expression.
Molecular Weight

472.53

Formula

C24H32N4O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(OC(C)(C)C)NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=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 (211.63 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 2.1163 mL 10.5813 mL 21.1627 mL
5 mM 0.4233 mL 2.1163 mL 4.2325 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: 2.5 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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

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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 2.1163 mL 10.5813 mL 21.1627 mL 52.9067 mL
5 mM 0.4233 mL 2.1163 mL 4.2325 mL 10.5813 mL
10 mM 0.2116 mL 1.0581 mL 2.1163 mL 5.2907 mL
15 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5271 mL
20 mM 0.1058 mL 0.5291 mL 1.0581 mL 2.6453 mL
25 mM 0.0847 mL 0.4233 mL 0.8465 mL 2.1163 mL
30 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7636 mL
40 mM 0.0529 mL 0.2645 mL 0.5291 mL 1.3227 mL
50 mM 0.0423 mL 0.2116 mL 0.4233 mL 1.0581 mL
60 mM 0.0353 mL 0.1764 mL 0.3527 mL 0.8818 mL
80 mM 0.0265 mL 0.1323 mL 0.2645 mL 0.6613 mL
100 mM 0.0212 mL 0.1058 mL 0.2116 mL 0.5291 mL
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Thalidomide-NH-C6-NH-Boc 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:

Thalidomide-NH-C6-NH-Boc2093536-13-9E3 Ligase Ligand-Linker ConjugatesAutophagyApoptosisMI389PROTACKasumi-1leukemiaAMLT-AMLCCRF-CEMJURKATMOLT4Inhibitorinhibitorinhibit

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