2361988-77-2

2361988-77-2 structure
2361988-77-2 structure
  • Name: cRIPGBM chloride
  • Chemical Name: cRIPGBM chloride
  • CAS Number: 2361988-77-2
  • Molecular Formula: C26H20ClFN2O2
  • Molecular Weight: 446.90
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2023-05-19 10:18:43
  • Modify Date: 2025-09-29 17:45:19
  • cRIPGBM(chloride), an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models[1].

Name cRIPGBM chloride
Description cRIPGBM(chloride), an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models[1].
Related Catalog
Target

Caspase-1

RIPK2

In Vitro cRIPGBM(chloride) (0.25 μM;0-24 小时) 时间依赖性地激活半胱天冬酶 1、半胱天冬酶 9 和半胱天冬酶 7,以及 PARP 裂解[1]。 cRIPGBM(chloride) (0.125 μM, 0.25 μM;24 小时) 在 CBM-1 GBM CSCs[1] 中诱导 caspase 1 介导的细胞凋亡[1]。 Western Blot Analysis[1] Cell Line: GBM-1 GBM CSCs Concentration: 50 nM, 100 nM, 125 nM, 250 nM, and 500 nM Incubation Time: 3 h, 6 h, 12 h, and 24 h Result: Had the ability to regulate RIPK2 to act as a prosurvival or proapoptotic molecule. Significantly reduced RIPK2 binding to cIAP2 in a dose-dependent manner.
In Vivo cRIPGBM(chloride) (50 mg/kg;口服;每天两次,持续 5 周) 在携带患者来源的 GBM CSC 颅内异种移植的小鼠模型再,抑制肿瘤生长[1]。 Animal Model: Orthotopic intracranial xenograft model in mouse[1] Dosage: 50 mg/kg Administration: PO; twice daily, 8 h apart, starting at day 7 postinjection; last for 5 weeks Result: Monitored by Fluorescence Tomography System. Decreased the tumor signal, as well as tumor size.
References

[1]. Lucki NC, et al. A cell type-selective apoptosis-inducing small molecule for the treatment of brain cancer. Proc Natl Acad Sci U S A. 2019 Mar 26;116(13):6435-6440.  

Molecular Formula C26H20ClFN2O2
Molecular Weight 446.90
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