| Identification | Back Directory | [Name]
Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- | [CAS]
920650-00-6 | [Synonyms]
Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)-
NCGC-00378430,Inhibitor,T47D,E-CAD,MCF7,Phosphatase,NCGC 00378430,TGF-β,inhibit,NCGC00378430,SIX1,p-Smad3,breast,EMT,cancer,FN1,transcriptional,EYA2 | [Molecular Formula]
C22H23N3O5S | [MOL File]
920650-00-6.mol | [Molecular Weight]
441.5 |
| Hazard Information | Back Directory | [Uses]
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model[1]. | [in vivo]
NCGC00378430 (25 mg/kg; local injection to the site of tumor; every other day; from day 3 until the day 21) dramatically decreases distant metastatic burden compared to vehicle treatment[1].
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NCGC00378430 (20 mg/kg; IV) has a T1/2α of 0.25 hours[1].
| Animal Model: | 6-8 week old NSG mice with MCF7 tumor cells[1] | | Dosage: | 25 mg/kg | | Administration: | Local Injection to the site of tumor; every other day; from day 3 until the day 21 | | Result: | Dramatically decreased distant metastatic burden compared to vehicle treatment.
Had no growth inhibitory effect.
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| Animal Model: | Mice[1] | | Dosage: | 20 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV | | Result: | Had a T1/2α of 0.25 hours, a CL of 6.19 L/hr?kg, a Vss of 4.08 L/kg, a Cmax of 6703 ng/mL and an AUC of 3234 ng/mL?hr.
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| [References]
[1] Hengbo Zhou, et al. Identification of a Small-Molecule Inhibitor That Disrupts the SIX1/EYA2 Complex, EMT, and Metastasis. Cancer Res. 2020 Jun 15;80(12):2689-2702. DOI:10.1158/0008-5472.CAN-20-0435 |
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