SML3882

DU-14

≥95% (HPLC)

• Synonym(s): ((4-((S)-3-(((S)-6-(3-Bromo-4-methylbenzamido)-1-((3-(2-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethyl)benzyl)amino)-1-oxohexan-2-yl)amino)-2-((S)-2-(2-(4-hydroxy-3-methoxyphenyl)acetamido)-3-phenylpropanamido)-3-oxopropyl)phenyl)difluoromethyl)phosphonic acid, DU 14, DU14
• Empirical Formula (Hill Notation): C₇₄H₈₅BrF₂N₉O₁₄PS
• Molecular Weight: 1505.46
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: (Powder or Lyophilized powder or film)
• color: white to off-white
• storage temp.: -10 to -25°C

Description

Biochem/physiol Actions

VHL E3 ligase-dependent, highly potent and selective dual degrader of cellular PTP1B and TC-PTP (TCPTP) with anti-tumor efficacy in vivo.


DU-14 is a VHL E3 ligase-dependent, highly potent and selective dual degrader of PTP1B and TC-PTP (PTP1B/TCPTP DC50 post 16h treatment from 4.3/4.4 nM to 67.4/62.5 nM among 10 cell lines; 95% PTP1B & 92% TC-PTP degradation in HEK293 cells post 16h at 200 nM) with 88/162/302/342-fold selectivity over PTP-Meg2/FAP1/CD45/SHP2 and >400-fold over 8 other PTPs. DU-14 promotes CD8+ T-cell activation (48h 1 nM treatment prior to stimulation by α-CD3/α-CD28; murine CD8+ T-cells) and increases IFN-γ signaling (16h 25-500 nM treatment prior to IFN-γ stimulation; MC38 & U2OS cells). DU-14 blocks MC38 tumor growth in a syngeneic mouse model in vivo (25 or 50 mg/kg i.p.).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable