For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I045124 |
| CAS Number | 2624313-15-9 |
| Synonyms | [(1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[[7-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-7-oxoheptyl]amino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate;2,2,2-trifluoroacetic acid |
| Molecular Formula | C70H91F3N6O16S |
| Purity | ≥95% |
| InChI | InChI=1S/C68H90N6O14S.C2HF3O2/c1-12-49(47-36-57(84-9)61(86-11)58(37-47)85-10)65(79)73-34-20-18-22-51(73)67(81)88-54(31-25-44-26-32-55(82-7)56(35-44)83-8)50-21-16-17-23-53(50)87-40-60(77)69-33-19-14-13-15-24-59(76)72-63(68(4,5)6)66(80)74-39-48(75)38-52(74)64(78)71-42(2)45-27-29-46(30-28-45)62-43(3)70-41-89-62;3-2(4,5)1(6)7/h16-17,21,23,26-30,32,35-37,41-42,48-49,51-52,54,63,75H,12-15,18-20,22,24-25,31,33-34,38-40H2,1-11H3,(H,69,77)(H,71,78)(H,72,76);(H,6,7)/t42-,48+,49-,51-,52-,54+,63+;/m0./s1 |
| InChIKey | KSEWNBIDXKMTNT-LNVAYBNASA-N |
| SMILES | CCC(C1=CC(=C(C(=C1)OC)OC)OC)C(=O)N2CCCCC2C(=O)OC(CCC3=CC(=C(C=C3)OC)OC)C4=CC=CC=C4OCC(=O)NCCCCCCC(=O)NC(C(=O)N5CC(CC5C(=O)NC(C)C6=CC=C(C=C6)C7=C(N=CS7)C)O)C(C)(C)C.C(=O)(C(F)(F)F)O |
| Reference | [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. |
