1. PROTAC Cell Cycle/DNA Damage Autophagy Apoptosis Immunology/Inflammation
  2. PROTACs FKBP
  3. dTAGV-1

dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)).

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dTAGV-1

dTAGV-1 Chemical Structure

CAS No. : 2451573-86-5

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Description

dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A))[1].

In Vitro

dTAGV-1 (0.1 nM-10 μM; 24 h) induces potent degradation of FKBP12F36V-Nluc with no effects on FKBP12WT-Nluc in 293FT cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

dTAGV-1 (35 mg/kg; i.p; 3 days) TFA induces degradation of FKBP12F36V-Nluc in mice[1].
Pharmacokinetic Analysis in Mice (non-salt form)[1]

Route Dose (mg/kg) Tmax (hr) t1/2 (hr) Cmax (ng/mL) AUClast (hr·ng/mL) AUCinf (hr·ng/mL) CL (mL/min/kg) Vss (L/kg)
i.v. 2 0.08 3.02 7780 3245 3329 10.1 0.56
i.p. 10 2.00 4.43 2123 18088 18517 9.05 /
i.p. 2 1.67 3.64 595 2245 3136 10.7 /

MedChemExpress (MCE) 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: Intraperitoneal injection (i.p.); once daily for 3 days
Result: Significantly reduced the bioluminescent signal 4 h after the first administration. The signal continuously decreased 4 h after each of the three administrations, and degradation was still evident 28 h after the final administration.
Molecular Weight

1247.54

Formula

C68H90N6O14S

CAS No.
SMILES

O=C([C@H]1N(CCCC1)C([C@H](C2=CC(OC)=C(C(OC)=C2)OC)CC)=O)O[C@@H](C3=C(C=CC=C3)OCC(NCCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)CCC7=CC(OC)=C(C=C7)OC

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
dTAGV-1
Cat. No.:
HY-145514D
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