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T-025

Chemical Structure : T-025

CAS No.: 2407433-00-3

T-025 (T025;CLK inhibitor T-025)

Catalog No.: PC-35047Not For Human Use, Lab Use Only.

T-025 (T025, CLK inhibitor T-025) is an orally available, potent inhibitor of Cdc2-like kinases (CLKs) with Kd of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, also inhibits DYRK1A and DYRK1B with IC50 of 0.074 and 1.5 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

T-025 (T025, CLK inhibitor T-025) is an orally available, potent inhibitor of Cdc2-like kinases (CLKs) with Kd of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, also inhibits DYRK1A and DYRK1B with IC50 of 0.074 and 1.5 nM.
T-025 (T025, CLK inhibitor T-025) reduces CLK-dependent phosphorylation, induces skipping exon, resulting in anti-proliferative effect in MDA-MB-468 in vitro and in vivo accompanied by the modulation of pre-mRNA splicing.
T-025 (T025, CLK inhibitor T-025) shows sensitivity against high CLK2 expression or MYC amplification cancer celles.
T-025 (T025, CLK inhibitor T-025) exhibits significant anti-tumor efficacy in MYC-driven breast tumor allograft models.

Physicochemical Properties

M.Wt 382.431
Formula C21H18N8
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N2-methyl-N4-(pyrimidin-2-ylmethyl)-5-(quinolin-6-yl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine

References

1. Iwai K, et al. EMBO Mol Med. 2018 May 16. pii: e8289.

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