2. Cell Cycle/DNA Damage Apoptosis Protein Tyrosine Kinase/RTK
  3. CDK Apoptosis DYRK
  4. T025

T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research.

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

T025 Chemical Structure

T025 Chemical Structure

CAS No. : 2407433-00-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

T025 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research[1].

IC50 & Target

CLK2

0.096 nM (Kd)

CLK4

0.61 nM (Kd)

CLK1

4.8 nM (Kd)

CLK3

6.5 nM (Kd)

DYRK1A

0.074 nM (Kd)

DYRK1B

1.5 nM (Kd)

DYRK2

32 nM (Kd)

In Vitro

T025 (0-1000 nM; 72 hours) significantly suppresses the growth of MDA-MB-468 cells in a dose-dependent manner[1].
T025 (0-1000 nM; 6 hours) reduces phosphorylation levels in MDA-MB-468 cells[1].

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

T025 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 72 hours
Result: Resulted in concentration dependent growth inhibition.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 10, 30, 100, 300 and 1000 nM
Incubation Time: 6 hours
Result: Decreased both pCLK2 and CLK2.
In Vivo

T025 (50 mg/kg; p.o.; 2, 4, 8 hours, Balb/c nude mice (7 to 8 week-old females).) suppress the CLK-dependent phosphorylation and induce skipping exon in various genes[1].
T025 (50 mg/kg; p.o.; twice daily on 2 days per week, for 3 weeks, Balb/c nude mice (7 to 8 week-old females).) inhibits MDA-MB-468 xenograft mice tumor growth and without affect body weight [1].

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

Animal Model: Balb/c nude mice (7 to 8 week-old females)[1]
Dosage: 50 mg/kg
Administration: Oral administration; 2, 4, 8 hours.
Result: pCLK2 detected with immunohistochemistry and immunoblotting decreased, by a reduction in the RPS6KB1 exon 7 and BCLAF1 exon 11 percentage splice-in (PSI) values.
Animal Model: Balb/c nude mice (7 to 8 week-old females)[1]
Dosage: 50 mg/kg
Administration: Oral administration; twice daily on 2 days per week, for 3 weeks.
Result: Suppressed tumor growth and < 10% nadir body weight loss.
Molecular Weight

382.42

Formula

C21H18N8
CAS No.
Appearance

Solid

Color

Yellow to green

SMILES

CNC1=NC(NCC2=NC=CC=N2)=C(C(C3=CC=C(N=CC=C4)C4=C3)=CN5)C5=N1
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 : 8.25 mg/mL (21.57 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 2.6149 mL 13.0746 mL 26.1493 mL
5 mM 0.5230 mL 2.6149 mL 5.2299 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (26.15 mM); Suspended solution; Need ultrasonic and warming and heat to 40°C

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.84%

COA (260 KB) HNMR (217 KB) LCMS (141 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 2.6149 mL 13.0746 mL 26.1493 mL 65.3731 mL
5 mM 0.5230 mL 2.6149 mL 5.2299 mL 13.0746 mL
10 mM 0.2615 mL 1.3075 mL 2.6149 mL 6.5373 mL
15 mM 0.1743 mL 0.8716 mL 1.7433 mL 4.3582 mL
20 mM 0.1307 mL 0.6537 mL 1.3075 mL 3.2687 mL
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T025 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:

T0252407433-00-3T 025T-025CDKApoptosisDYRKCyclin dependent kinaseDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseCdc2-like kinasesCLKsCaspase-3/7Inhibitorinhibitorinhibit

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