SML3882
DU-14
≥95% (HPLC)
别名:
((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
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关于此项目
经验公式（希尔记法）:
C74H85BrF2N9O14PS
分子量:
1505.46
NACRES:
NA.77
UNSPSC Code:
12352200
Quality Level
assay
≥95% (HPLC)
form
(Powder or Lyophilized powder or film)
color
white to off-white
storage temp.
-10 to -25°C
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.).
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.).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Small Molecule Degraders of Protein Tyrosine Phosphatase 1B and T-Cell Protein Tyrosine Phosphatase for Cancer Immunotherapy
Angewandte Chemie (International Edition in English), 62(22) (2023)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML3882-5MG | 04065270573834 |
| SML3882-1MG | 04065270573827 |
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