T-025
- Product Name
- T-025
- CAS No.
- 2407433-00-3
- Chemical Name
- T-025
- Synonyms
- T-025;T13058;T025,T-025;T025, 10 mM in DMSO;N2-Methyl-N4-(pyrimidin-2-ylmethyl)-5-(quinolin-6-yl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine;7H-Pyrrolo[2,3-d]pyrimidine-2,4-diamine, N2-methyl-N4-(2-pyrimidinylmethyl)-5-(6-quinolinyl)-;N2-Methyl-N4-(pyrimidin-2-ylmethyl)-5-(quinolin-6-yl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine , T025
- CBNumber
- CB24668567
- Molecular Formula
- C21H18N8
- Formula Weight
- 382.42
- MOL File
- 2407433-00-3.mol
T-025 Property
- Density
- 1.432±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 8.25 mg/mL (21.57 mM; Need ultrasonic)
- pka
- 13.45±0.50(Predicted)
- form
- Solid
- color
- Yellow to green
N-Bromosuccinimide Price
- Product number
- CS-0044754
- Product name
- T025
- Purity
- 98.61%
- Packaging
- 5mg
- Price
- $450
- Updated
- 2021/12/16
T-025 Chemical Properties,Usage,Production
Uses
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].
Biological Activity
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]. 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]. 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].
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].
| 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. |
IC 50
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)
References
[1]. Iwai K, et al. Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability. EMBO Mol Med. 2018 Jun;10(6):e8289.
T-025 Preparation Products And Raw materials
Raw materials
Preparation Products
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