2. PROTAC
  3. Ligands for E3 Ligase
  4. TD-106

TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.

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

TD-106 Chemical Structure

TD-106 Chemical Structure

CAS No. : 2250288-69-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1950 In-stock
100 mg USD 2950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TD-106 Related Antibodies

Top Publications Citing Use of Products

View All Ligands for E3 Ligase Isoform Specific Products:

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation[1].

IC50 & Target

CRBN[1]
Cellular Effect
Cell Line Type Value Description References
NCI-H929 CC50
0.039 μM
Compound: TD-106; 4a
Antiproliferative activity against human NCI-H929 cells after 72 hrs by WST-1 assay
Antiproliferative activity against human NCI-H929 cells after 72 hrs by WST-1 assay
[PMID: 30684871]
In Vitro

TD-106 (0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10 μM, and 100 μM; 72 hours) inhibits the proliferation of NCI-H929 myeloma cell line with an CC50 of 0.039 μM[1].
TD-106 (1, 10, 100, and 1000 nM) induces the degradation of IKZF1/3 in NCI-H929 cells[1].

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

TD-106 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: NCI-H929 cells
Concentration: 72 hours
Incubation Time: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM, 10 μM, and 100 μM
Result: Inhibited cell proliferation with an CC50 of 0.039 μM.
In Vivo

TD-106 (50 mg/kg; intraperitoneally; q.d. for 14 days) possesses anti-myeloma activity in SCID mice with TMD-8 xenograft model.

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

Animal Model: Female SCID (CB-17/IcrCri-scid) mice with TMD-8 xenograft model[1]
Dosage: 50 mg/kg
Administration: Intraperitoneally (i.p.); q.d. for 14 days
Result: Treatment inhibited tumor growth during this duration.
Molecular Weight

273.25

Formula

C12H11N5O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=CC=CC(N=NN2C3CCC(NC3=O)=O)=C1C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (457.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6597 mL 18.2983 mL 36.5965 mL
5 mM 0.7319 mL 3.6597 mL 7.3193 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 (9.15 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 (9.15 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

Purity: 98.67%

SDS (393 KB)

COA (252 KB) RP-HPLC (207 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6597 mL 18.2983 mL 36.5965 mL 91.4913 mL
5 mM 0.7319 mL 3.6597 mL 7.3193 mL 18.2983 mL
10 mM 0.3660 mL 1.8298 mL 3.6597 mL 9.1491 mL
15 mM 0.2440 mL 1.2199 mL 2.4398 mL 6.0994 mL
20 mM 0.1830 mL 0.9149 mL 1.8298 mL 4.5746 mL
25 mM 0.1464 mL 0.7319 mL 1.4639 mL 3.6597 mL
30 mM 0.1220 mL 0.6099 mL 1.2199 mL 3.0497 mL
40 mM 0.0915 mL 0.4575 mL 0.9149 mL 2.2873 mL
50 mM 0.0732 mL 0.3660 mL 0.7319 mL 1.8298 mL
60 mM 0.0610 mL 0.3050 mL 0.6099 mL 1.5249 mL
80 mM 0.0457 mL 0.2287 mL 0.4575 mL 1.1436 mL
100 mM 0.0366 mL 0.1830 mL 0.3660 mL 0.9149 mL
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TD-106 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:

TD-1062250288-69-6TD106TD 106Ligands for E3 LigaseE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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