dTAGV-1 TFA

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dTAGV-1 TFA 

dTAGV-1 TFA 是一种有效和选择性的突变 FKBP12F36V 融合蛋白降解剂。dTAGV-1 TFA 可以在体内诱导 FKBP12F36V-Nluc 降解。

dTAGV-1 TFA

dTAGV-1 TFA Chemical Structure

CAS No. : 2624313-15-9

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生物活性

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].

IC50 & Target[1]

VHL

 

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

1361.56

Formula

C70H91F3N6O16S
CAS 号

2624313-15-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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