Description
(S, R, S)-AHPC TFA (VH032-NH2 TFA) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S, R, S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
Product information
CAS Number: 1631137-51-3
Molecular Weight: 544.59
Formula: C24H31F3N4O5S
Synonym:
VH032-NH2 TFA
VHL ligand 1 TFA
Chemical Name: (2S, 4R)-1-[(2S)-2-amino-3, 3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide; trifluoroacetic acid
Smiles: CC(C)(C)[C@H](N)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC1C=CC(=CC=1)C1SC=NC=1C.OC(=O)C(F)(F)F
InChiKey: SGNZARGJXDPTDJ-MSSRUXLCSA-N
InChi: InChI=1S/C22H30N4O3S.C2HF3O2/c1-13-18(30-12-25-13)15-7-5-14(6-8-15)10-24-20(28)17-9-16(27)11-26(17)21(29)19(23)22(2,3)4;3-2(4,5)1(6)7/h5-8,12,16-17,19,27H,9-11,23H2,1-4H3,(H,24,28);(H,6,7)/t16-,17+,19-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Buckley DL, et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.
Products are for research use only. Not for human use.
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