1. Apoptosis
  2. RIP kinase Caspase Apoptosis
  3. cRIPGBM chloride

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.

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cRIPGBM chloride Chemical Structure

cRIPGBM chloride Chemical Structure

CAS No. : 2361988-77-2

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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

Caspase-1

 

RIPK2

 

In Vitro

cRIPGBM chloride (0.25 μM; 0-24 h) time-dependently activates caspase 1, caspase 9, and caspase 7, as well as PARP cleavage, in CBM-1 GBM CSCs[1].
cRIPGBM chloride (0.125 μM, 0.25 μM; 24 h) induces cell apoptosis mediated by caspase 1 in CBM-1 GBM CSCs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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; p.o.; twice daily for 5 weeks) inhibits tumor growth in patient-derived GBM CSC intracranial xenograft mouse models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

446.90

Formula

C26H20ClFN2O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C2[N+](CC3=CC=C(F)C=C3)=C(C)N1CC4=CC=CC=C4)C5=C(C=CC=C5)C2=O.[Cl-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.94 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2376 mL 11.1882 mL 22.3764 mL
5 mM 0.4475 mL 2.2376 mL 4.4753 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2376 mL 11.1882 mL 22.3764 mL 55.9409 mL
5 mM 0.4475 mL 2.2376 mL 4.4753 mL 11.1882 mL
10 mM 0.2238 mL 1.1188 mL 2.2376 mL 5.5941 mL
15 mM 0.1492 mL 0.7459 mL 1.4918 mL 3.7294 mL
20 mM 0.1119 mL 0.5594 mL 1.1188 mL 2.7970 mL
25 mM 0.0895 mL 0.4475 mL 0.8951 mL 2.2376 mL
30 mM 0.0746 mL 0.3729 mL 0.7459 mL 1.8647 mL
40 mM 0.0559 mL 0.2797 mL 0.5594 mL 1.3985 mL
50 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
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cRIPGBM chloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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cRIPGBM chloride
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