dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12 fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12-Nluc in vivo.
性状
Solid
IC50 & Target[1][2]
VHL
体外研究(In Vitro)
dTAGV-1 (0.1 nM-10 μM; 24 h) TFA induces potent degradation of FKBP12-Nluc with no effects on FKBP12-Nluc in 293FT cells.dTAGV-1 (125-2000 nM; 24 h) TFA co-treatment with THAL-SNS-032 leads to pronounced degradation of both LACZ-FKBP12 and CDK9.dTAGV-1 (500 nM; 1-24 h) TFA leads to rapid KRAS and pERK1/2 degradation.dTAGV-1 (50-5000 nM; 24 h) TFA enables EWS/FLI degradation in Ewing sarcoma. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
dTAGV-1 (35 mg/kg; i.p. once daily for 4 days) TFA induces degradation of FKBP12-Nluc in mice.
dTAGV-1 (2-10 mg/kg; i.p.) TFA exhbits half-lives (T 1/2 =3.64 and 4.4 h), C max (595 and 2123 ng/mL) and great exposure (AUC inf ?=3136 and?18517 h?ng/mL) in mice.
dTAGV-1 (2 mg/kg; i.v.) TFA exhbits half-life (T 1/2 =3.02 h), C max (7780 ng/mL) and great exposure (AUC inf ?=3329 h?ng/mL) in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Nabet B, et, al. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat Commun. 2020 Sep 18;11(1):4687.
溶解度数据
In Vitro: DMSO : 37.5 mg/mL (27.54 mM; Need ultrasonic)配制储备液