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T-1101 tosylate

Chemical Structure : T-1101 tosylate

CAS No.: 2250404-95-4

T-1101 tosylate (TAI-95 tosylate)

Catalog No.: PC-20310Not For Human Use, Lab Use Only.

T-1101 tosylate (TAI-95 tosylate) is a potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).

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Biological Activity

T-1101 tosylate (TAI-95 tosylate) is a potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).
T-1101 tosylate demonstrates strong inhibition of in vivo tumor growth of breast cancer models without inducing weight loss or other obvious toxicity.
T-1101 tosylate induces apoptotic cell death, shows activity on MDR cell lines and leads to downregulation of the expression of P-glycoprotein (Pgp),.
T-1101 tosylate also increases the potency of cytotoxic Pgp substrates, including doxorubicin and topotecan.
T-1101 tosylate showed promise in antitumor activity in mice bearing human tumor xenografts of liver cancer (Huh-7), as well as of breast cancer (BT474, MDA-MB-231, and MCF7) with oral administration.

Physicochemical Properties

M.Wt 665.80
Formula C31H31N5O6S3
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

N-[4-(4-{[5-(2-methoxyethoxy)pyrazine-2-yl]thio}-2,6-dimethylphenyl) thiazol-2-yl]isonicotinamide tosylate

References

1. Huang LY, et al. Mol Cancer Ther. 2014 Jun;13(6):1419-30.

2. Chuang SH, et al. Eur J Med Chem. 2020 Apr 1;191:112118.

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