| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C, away from moisture and light | [solubility ]
DMSO : 37.5 mg/mL (27.54 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to light brown |
| Hazard Information | Back Directory | [Uses]
dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12F36V-Nluc in vivo[1]. | [in vivo]
dTAGV-1 (35 mg/kg; i.p. once daily for 4 days) TFA induces degradation of FKBP12F36V-Nluc in mice[1].
dTAGV-1 (2-10 mg/kg; i.p.) TFA exhbits half-lives (T1/2=3.64 and 4.4 h), Cmax (595 and 2123 ng/mL) and great exposure (AUCinf?=3136 and?18517 h?ng/mL) in mice[1].
dTAGV-1 (2 mg/kg; i.v.) TFA exhbits half-life (T1/2=3.02 h), Cmax (7780 ng/mL) and great exposure (AUCinf?=3329 h?ng/mL) in mice[1].
| Animal Model: | 8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12F36V cells[1] | | Dosage: | 35 mg/kg | | Administration: | I.p. once daily for 4 days | | Result: | Observed striking loss of bioluminescent signal 4?h after the first and three administrations.
Degradation evident 28?h after the final administration.
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| [IC 50]
VHL | [storage]
Store at -20°C, away from moisture and light | [References]
[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. DOI:10.1038/s41467-020-18377-w |
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