2. Cell Cycle/DNA Damage
  3. CDK
  4. CTX-712

CTX-712 is an orally effective CLK 2 inhibitor, with an IC50 of 1.4 nM, showing anti-tumor activity.

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

CTX-712 Chemical Structure

CTX-712 Chemical Structure

CAS No. : 2144751-78-8

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Customer Review

Based on 1 publication(s) in Google Scholar

CTX-712 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CTX-712 is an orally effective CLK 2 inhibitor, with an IC50 of 1.4 nM, showing anti-tumor activity[1][2].

IC50 & Target

CLK2

1.4 nM (IC50)

In Vitro

CTX-712 has a strong inhibitory effect on the proliferation of human myeloid K562 and MV-4-11 cells, with an IC50 of 0.15 and 0.036 μM, respectively. For primary acute myeloid leukemia (AML) cells, the IC50 is 0.078 μM, demonstrating its anti-leukemia activity[1].
CTX-712 inhibits the phosphorylation of various serine/arginine (SR) proteins, including SRSF3/4/6, which can interact with SRSF2[1].

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

CTX-712 Related Antibodies
In Vivo

CTX-712 (6.25-12.5 mg/kg, orally, for two weeks) reduces tumor size and increases survival rates in mice with myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML) [1].

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

Animal Model: Mouse models of myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML). [1]
Dosage: 6.25, 12.5 mg/kg, two weeks
Administration: Oral
Result: Showed two cases of SRSF2 mutations, P95H and P95L observed with significant dose-dependent effects. P95H reduced tumor volume and improved survival rates in the SRSF2 P95L model.
Clinical Trial
Molecular Weight

408.39

Formula

C19H17FN8O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC2=NC=C(C3=C4C(OC)=NC=NN4C=C3)C=C2N1CC5=NN=C([C@H](F)C)O5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (61.22 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 2.4486 mL 12.2432 mL 24.4864 mL
5 mM 0.4897 mL 2.4486 mL 4.8973 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 (sealed storage, away from moisture and light). 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
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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 (6.12 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 (6.12 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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 (sealed storage, away from moisture and light). 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 2.4486 mL 12.2432 mL 24.4864 mL 61.2160 mL
5 mM 0.4897 mL 2.4486 mL 4.8973 mL 12.2432 mL
10 mM 0.2449 mL 1.2243 mL 2.4486 mL 6.1216 mL
15 mM 0.1632 mL 0.8162 mL 1.6324 mL 4.0811 mL
20 mM 0.1224 mL 0.6122 mL 1.2243 mL 3.0608 mL
25 mM 0.0979 mL 0.4897 mL 0.9795 mL 2.4486 mL
30 mM 0.0816 mL 0.4081 mL 0.8162 mL 2.0405 mL
40 mM 0.0612 mL 0.3061 mL 0.6122 mL 1.5304 mL
50 mM 0.0490 mL 0.2449 mL 0.4897 mL 1.2243 mL
60 mM 0.0408 mL 0.2041 mL 0.4081 mL 1.0203 mL
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CTX-712 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:

CTX-7122144751-78-8CTX712CTX 712CDKCyclin dependent kinaseCdc2-like kinaseCLKCancer survivalCancer cell growthInhibitorinhibitorinhibit

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