2624313-15-9
2624313-15-9 structure
- Name: dTAGV-1 TFA
- Chemical Name: dTAGV-1 TFA
- CAS Number: 2624313-15-9
- Molecular Formula: C70H91F3N6O16S
- Molecular Weight: 1361.56
- Catalog: Signaling Pathways PROTAC PROTAC
- Create Date: 2022-03-28 12:18:33
- Modify Date: 2024-01-11 21:40:58
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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].
| Name | dTAGV-1 TFA |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
VHL |
| In Vitro | dTAGV-1 (0.1 nM-10 μM; 24 h) TFA induces potent degradation of FKBP12F36V-Nluc with no effects on FKBP12WT-Nluc in 293FT cells[1]. dTAGV-1 (125-2000 nM; 24 h) TFA co-treatment with THAL-SNS-032 leads to pronounced degradation of both LACZ-FKBP12F36V and CDK9[1]. dTAGV-1 (500 nM; 1-24 h) TFA leads to rapid KRASG12V and pERK1/2 degradation[1]. dTAGV-1 (50-5000 nM; 24 h) TFA enables EWS/FLI degradation in Ewing sarcoma[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. |
| References |
| Molecular Formula | C70H91F3N6O16S |
|---|---|
| Molecular Weight | 1361.56 |