1. Cell Cycle/DNA Damage
  2. CDK
  3. THZ1-R

THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.

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

THZ1-R Chemical Structure

THZ1-R Chemical Structure

CAS No. : 1621523-07-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 508 In-stock
Solution
10 mM * 1 mL in DMSO USD 508 In-stock
Solid
1 mg USD 198 In-stock
5 mg USD 462 In-stock
10 mg USD 726 In-stock
50 mg USD 2178 In-stock
100 mg USD 3036 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of THZ1-R:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.

IC50 & Target[1]

CDK7

146 nM (IC50)

In Vitro

THZ1-R shows lower affinity at CDK7 than THZ1, with IC50 of 146 nM[1].

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

Molecular Weight

568.07

Formula

C31H30ClN7O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CN=C(NC2=CC(NC(C3=CC=C(NC(CCCN(C)C)=O)C=C3)=O)=CC=C2)N=C1C4=CNC5=CC=CC=C54

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (176.03 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 1.7603 mL 8.8017 mL 17.6035 mL
5 mM 0.3521 mL 1.7603 mL 3.5207 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 (4.40 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 98.12%

References
Cell Assay
[1]

Cells are seeded in 384-well microplates at 15% confluency in medium with 5% FBS and penicillin/streptavidin. Cells are treated with THZ1 or DMSO for 72 hrs and cell viability is determined using resazurin.

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

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 1.7603 mL 8.8017 mL 17.6035 mL 44.0087 mL
5 mM 0.3521 mL 1.7603 mL 3.5207 mL 8.8017 mL
10 mM 0.1760 mL 0.8802 mL 1.7603 mL 4.4009 mL
15 mM 0.1174 mL 0.5868 mL 1.1736 mL 2.9339 mL
20 mM 0.0880 mL 0.4401 mL 0.8802 mL 2.2004 mL
25 mM 0.0704 mL 0.3521 mL 0.7041 mL 1.7603 mL
30 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.4670 mL
40 mM 0.0440 mL 0.2200 mL 0.4401 mL 1.1002 mL
50 mM 0.0352 mL 0.1760 mL 0.3521 mL 0.8802 mL
60 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7335 mL
80 mM 0.0220 mL 0.1100 mL 0.2200 mL 0.5501 mL
100 mM 0.0176 mL 0.0880 mL 0.1760 mL 0.4401 mL
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THZ1-R 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.

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THZ1-R
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