Structure of NT157
CAS No.: 1384426-12-3
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
NT157 treatment resulted in dose-dependent inhibition of IGF1R activation, suppression of IRS protein expression, inhibition of IGF1-induced AKT activation, but increased ERK activation in NT157-treated cells in vitro.
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CAS No. : | 1384426-12-3 |
Formula : | C16H14BrNO5S |
M.W : | 412.26 |
SMILES Code : | S=C(NCC1=CC(O)=C(O)C(O)=C1)/C=C/C2=CC(O)=C(O)C(Br)=C2 |
MDL No. : | MFCD28127272 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HCT-116 cells | 3 µM | 20 minutes | NT157 inhibited STAT3 phosphorylation | Oncogene. 2016 May 19;35(20):2634-44 |
MC-38 cells | 3 µM | 24 hours | NT157 inhibited IGF-1-induced ERK1/2 and AKT phosphorylation | Oncogene. 2016 May 19;35(20):2634-44 |
Cholinergic neurons | 10 µM | 2 hours | NT157 inhibits IRS1 and AKT phosphorylation, blocking NGF's activation of the insulin signaling pathway | Mol Neurobiol. 2019 Jan;56(1):535-552 |
MPC5 cells | 2 µM | 2 hours | NT157 treatment significantly reversed the protective effects of DOP on HG-treated MPC5 cells, showing markedly decreased glucose consumption, increased MDA production, reduced phosphorylation of IRS-1 and AKT, and increased DNA damage. | Aging (Albany NY). 2023 Oct 8;15(19):10291-10306 |
MEL-20-06-039 | 1 and 2.5 µM | 24 and 48 hours | RPPA protein profiling showed changes in PI3K/AKT pathway | Cancers (Basel). 2022 Dec 19;14(24):6247 |
MM28 | 1 and 2.5 µM | 24 and 48 hours | RPPA protein profiling showed changes in PI3K/AKT pathway | Cancers (Basel). 2022 Dec 19;14(24):6247 |
MEL270 | 1 and 2.5 µM | 24 and 48 hours | RPPA protein profiling showed changes in PI3K/AKT pathway | Cancers (Basel). 2022 Dec 19;14(24):6247 |
CAF cells | 3 µM | 24 hours | NT157 inhibited IGF-1-induced αSMA expression and collagen type I production | Oncogene. 2016 May 19;35(20):2634-44 |
SET2 cells | 0.2, 0.4, 0.8, 1.6, 3.2 µM | 24, 48, 72 hours | At high concentrations (3.2 μM), NT157 significantly reduced cell viability and induced apoptosis | Signal Transduct Target Ther. 2020 Jan 24;5(1):5 |
HEL cells | 0.2, 0.4, 0.8, 1.6, 3.2 µM | 24, 48, 72 hours | NT157 significantly reduced cell viability, increased apoptosis, inhibited cell proliferation and clonogenicity, and caused G2/M phase cell cycle arrest | Signal Transduct Target Ther. 2020 Jan 24;5(1):5 |
NCI-H460 | 1.6, 3.2, 6.4, 12.5, 25, 50, 100 µM | 24, 48, 72 hours | NT157 decreased cell viability in a time- and dose-dependent manner (p < 0.05). The IC50 ranged from 4.8 to 12.9 µM for H460 cells. | Sci Rep. 2022 Oct 12;12(1):17092 |
NCI-H1299 | 1.6, 3.2, 6.4, 12.5, 25, 50, 100 µM | 24, 48, 72 hours | NT157 decreased cell viability in a time- and dose-dependent manner (p < 0.05). The IC50 ranged from 1.7 to 9.7 µM for H1299 cells. | Sci Rep. 2022 Oct 12;12(1):17092 |
NCI-H1975 | 0.8, 1.6 µM | 48 hours | NT157 in combination with gefitinib presented potentiating effects in the reduction of cell viability of H1975 cells. | Sci Rep. 2022 Oct 12;12(1):17092 |
MP41 | 0.05, 0.1, 0.25, 0.5, 1.0, 2.5 µM | 72 hours | NT157 dose-dependent decrease in cell survival | Cancers (Basel). 2022 Dec 19;14(24):6247 |
MP65 | 0.05, 0.1, 0.25, 0.5, 1.0, 2.5 µM | 72 hours | NT157 dose-dependent decrease in cell survival | Cancers (Basel). 2022 Dec 19;14(24):6247 |
92.1 | 0.05, 0.1, 0.25, 0.5, 1.0, 2.5 µM | 72 hours | NT157 dose-dependent decrease in cell survival | Cancers (Basel). 2022 Dec 19;14(24):6247 |
MEL202 | 0.05, 0.1, 0.25, 0.5, 1.0, 2.5 µM | 72 hours | NT157 dose-dependent decrease in cell survival | Cancers (Basel). 2022 Dec 19;14(24):6247 |
MM28 | 0.05, 0.1, 0.25, 0.5, 1.0, 2.5 µM | 72 hours | NT157 dose-dependent decrease in cell survival | Cancers (Basel). 2022 Dec 19;14(24):6247 |
MP46 | 0.05, 0.1, 0.25, 0.5, 1.0, 2.5 µM | 72 hours | NT157 dose-dependent decrease in cell survival | Cancers (Basel). 2022 Dec 19;14(24):6247 |
U-2OS | 0.3–3 µM | 72 hours | Evaluate the inhibitory effect of NT157 on U-2OS cell proliferation, showing dose-dependent growth inhibition. | Front Endocrinol (Lausanne). 2015 May 13;6:74 |
OS-19 | 0.3–3 µM | 72 hours | Evaluate the inhibitory effect of NT157 on OS-19 cell proliferation, showing dose-dependent growth inhibition. | Front Endocrinol (Lausanne). 2015 May 13;6:74 |
MG-63 | 0.3–3 µM | 72 hours | Evaluate the inhibitory effect of NT157 on MG-63 cell proliferation, showing dose-dependent growth inhibition. | Front Endocrinol (Lausanne). 2015 May 13;6:74 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Chicken | Chicken chorioallantoic membrane (CAM) model | Topical application | 1 µM | Daily for 4 days | NT157 treatment reduces UM tumor growth | Cancers (Basel). 2022 Dec 19;14(24):6247 |
Balb/c mice | Methylated bovine serum albumin-immunised mice | Subcutaneous injection | 10 mg/kg | Mice were monitored daily throughout the experiment and sacrificed at the end (day 28) | Inhibition of IGF1R signaling led to enlargement of the marginal zone, increased frequency of IgM+CD21+B cells, and enhanced autoantibody production | Front Immunol. 2022 Aug 29;13:958206 |
Mice | Autologous blood injection-induced ICH model | Intraperitoneal injection | 50 mg/kg | Single dose, 1 hour before ICH | To investigate the reversal effect of NT157 on the protective effects of ELP, results showed that NT157 reversed the neurobehavioral improvement and anti-inflammatory effects of ELP. | J Cereb Blood Flow Metab. 2023 Jun;43(6):869-881 |
Mice | CPC-APC mouse model | Intraperitoneal injection | 70 mg/kg | Three times a week for 3-4 weeks | NT157 significantly reduced tumor burden, inhibited cancer cell proliferation and induced apoptosis, while also inhibiting CAF activation and inflammation | Oncogene. 2016 May 19;35(20):2634-44 |
Mice | 4T1 mammary tumor model | Intraperitoneal route | 70 mg/kg | Three times per week for 3 weeks | NT157 significantly decreased the number of metastatic lung nodules in 4T1 tumor-bearing mice and decreased expression of ARG1, TGFβ1, and IL-10 in sorted Gr-1+CD11b+ myeloid cells | Nat Commun. 2018 Jul 4;9(1):2611 |
Tags: NT157 | IGF-1R inhibitor | insulin-like growth factor 1 receptor antagonist | IRS1/2 degradation inducer | insulin receptor substrate 1 | insulin receptor substrate 2 | STAT3 signaling inhibitor | JAK/STAT pathway modulator | receptor tyrosine kinase pathway | apoptosis inducer | oncogenic signaling blockade | PI3K/AKT pathway modulation | 1384426-12-3 |
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