Top Suppliers:I want be here
Related CAS#:
181223-80-3 74067-99-5
85616-77-9 6078-46-2
13466-29-0 730-98-3
718-21-8 94864-83-2
102612-79-3 97669-69-7
1158522-08-7 940364-43-2
134104-43-1 131615-57-1
6906-52-1 540481-25-2
930439-75-1 1018584-77-4
1375289-11-4 849349-65-1

181223-80-3

181223-80-3 structure
181223-80-3 structure
  • Name: DEL 22379
  • Chemical Name: N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide
  • CAS Number: 181223-80-3
  • Molecular Formula: C26H28N4O3
  • Molecular Weight: 444.526
  • Catalog: Signaling Pathways MAPK/ERK Pathway ERK
  • Create Date: 2018-12-10 10:38:38
  • Modify Date: 2024-01-02 02:06:53
  • DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
Name N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide
Synonyms N-{(3Z)-3-[(5-Methoxy-1H-indol-3-yl)methylene]-2-oxo-2,3-dihydro-1H-indol-5-yl}-3-(1-piperidinyl)propanamide
DEL-22379
1-Piperidinepropanamide, N-[(3Z)-2,3-dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-
Description DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
Related Catalog
Target

ERK2:0.5 μM (IC50)

In Vitro DEL-22379 is an ERK dimerization inhibitor. DEL-22379 abolishes EGF-induced co-immunoprecipitation of ectopic ERK2 molecules tagged with hemagglutinin (HA) or FLAG epitopes, with an estimated half-maximal inhibitory concentration (IC50) of ~0.5 μM. DEL-22379 inhibits growth of tumor cells harboring RAS-ERK pathway oncogenes. The biological effects of DEL-22379 are investigated on tumor cells in culture. The cytostatic effects of DEL-22379 are compared to those of the MEK inhibitor PD-0325901 and the ERK kinase inhibitor SCH-772984, as reflected by their half-maximal growth inhibitory concentrations (GI50). Cell lines harboring mutant BRAF are the most sensitive to the three compounds. In comparison, wild-type (WT) cell lines for BRAF and RAS are the most resistant, and RAS mutant cells exhibit a range of sensitivities. In cells showing different oncogenic genotypes, distinct sensitivity to DEL-22379 can not be attributed to variations on its effects on dimerization, because DEL-22379 displays similar dimerization- and cytoplasmic signaling-inhibitory dose responses (IC50 of 150-400 nM) regardless of the genotype[1].
In Vivo To test DEL-22379 antitumor effects, some of the aforementioned cell lines are xenografted into nude mice, and tumor growth is monitored after intra-peritoneal administration of DEL-22379 at 15 mg/kg. At such a dose, inhibition of ERK dimerization is evident in liver extracts and in xenografted tumors. DEL-22379 markedly inhibits tumor progression for A375 cells (BRAF mutant)[1].
Cell Assay HEK293T cells are plated at a density of 1,000-2,000 cells/well and treated with DEL-22379 (0.2-1 μ M) for 48 hr, Alamar Blue is added, and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software. Apoptosis is analyzed by evaluating caspase 3 activity, either by western blotting or using the Caspase-Glo 3/7 luminogenic assay[1].
Animal Admin Mice[1] Cancer cells are xenografted in female, athymic nu/nu mice of 8 weeks of age. 3×106 cells are injected subcutaneously in the lateral flank and allowed to develop for 10-15 days before treatment with DEL-22379 at 15 mg/kg every 12 hr for 2 weeks. patient-derived xenografts (PDXs) are performed using patient-derived colorectal cancer cells harboring BRAFV600E from non-necrotic areas of primary adenocarcinomas from patients that undergo surgical resection. Cells are grafted in both flanks or in the cecum of NOD-SCID mice. DEL-22379 is administered by intra-peritoneal injection at a concentration of 15 mg/kg every 12 hr for 30 days[1].
References

[1]. Herrero A, et al. Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes. Cancer Cell. 2015 Aug 10;28(2):170-82.
Density 1.3±0.1 g/cm3
Boiling Point 763.9±60.0 °C at 760 mmHg
Molecular Formula C26H28N4O3
Molecular Weight 444.526
Flash Point 415.8±32.9 °C
Exact Mass 444.216156
LogP 3.13
Vapour Pressure 0.0±2.6 mmHg at 25°C
Index of Refraction 1.697
Storage condition -20℃

Chemsrc provides CAS#:181223-80-3 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 181223-80-3 | Chemsrc address: https://m.chemsrc.com/en/baike/1198641.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved