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

T025 

Cat. No.: HY-112296 Purity: 98.84%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 495 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE T025

  • 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].

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

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].

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

Appearance

Solid

Formula

C21H18N8

CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 8.25 mg/mL (21.57 mM; Need ultrasonic)

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
10 mM 0.2615 mL 1.3075 mL 2.6149 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation

Purity: 98.84%

References
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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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Product Name:
T025
Cat. No.:
HY-112296
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