VCP/p97 IN-4
VCP/p97 IN-4 is a p97/VCP inhibitor (Kd=14.99 μM) targeting the allosteric site of the D1-D2 domain. VCP/p97 IN-4 inhibits the ATPase activity of VCP/p97 in an ATP concentration-independent manner. VCP/p97 IN-4 induces apoptosis, autophagy, mitochondrial stress and mitochondrial membrane depolarization. VCP/p97 IN-4 inhibits the growth of patient-derived colorectal cancer organoids and exhibits in vivo efficacy in a colorectal cancer xenograft mouse model. VCP/p97 IN-4 can be used for the research of colorectal cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3114314-82-5
- Fòrmula: C28H29F2N3
- Peso molecular:445.55
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
In Vitro
VCP/p97 IN-4 (120 h) completely inhibits the growth of patient-derived colorectal cancer organoids (KOCO-092) with an IC50 of 5.35 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT-116, MC38, SW480, A549, 95D, 4T1, NB4, and Ketr-3
-
Concentration:0.19-100 μM
-
Incubation Time:48 h
-
Result:Potently inhibited proliferation of multiple cancer cell lines with IC50 values below 5 μM.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCINF_obs | MRTINF_obs |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 13.4 mg/kg | p.o. | 25.0 h | 1 h | 44.9 ng/mL | 780 ng·h/mL | 961 ng·h/mL | 36.8 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6N (female, 4-6 weeks old, 20-25 g, subcutaneous inoculation of MC38 colorectal cancer cells)[1]
-
Dosage:30 μmol/kg
-
Administration:i.p.; daily; 7 consecutive days
-
Result:Achieved 55% tumor growth inhibition rate.
Reduced mean final tumor weight to 0.45 g compared to control's 1.00 g.
Significantly reduced body weight compared to control group.
Significantly increased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels.
Showed no changes in kidney function markers (creatinine, urea).
Significantly reduced thymus/body weight ratio.
Decreased neutrophil counts.
- Annexin V plus membrane-impermeant dye apoptosis staining
- How to Choose the Right Model Animal
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Fluorescent plasma-membrane potential dye assay
- Autophagy
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Lysosome and acidic-vesicle live-cell staining
- Subcutaneous Cell-Line-Derived Xenograft
- Macroautophagy Solutions
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
-
No. CAS 3114314-82-5
-
Peso molecular 445.55
-
Fòrmula C28H29F2N3
-
SMILES
FC1=CC=C(C=C1)C(C2=CC=C(C=C2)F)CCCNC[C@@H]3CC4=C(NC5=C4C=CC=C5)CN3
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VCP/p97 IN-4 Related Classifications
HY-184291 Related Classifications
Powered by Bioz