Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- manufacturers
- NCGC00378430
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- $68.00 / 1mg
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2024-11-18
- CAS:920650-00-6
- Min. Order:
- Purity: 99.74%
- Supply Ability: 10g
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| Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- Basic information |
Product Name: | Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- | 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;N-(4-Methoxy-3-(morpholinosulfonyl)phenyl)-3-(1H-pyrrol-1-yl)benzamide;NCGC00378430, 10 mM in DMSO;N-[4-Methoxy-3-(morpholine-4-sulfonyl)phenyl]-3-(1H-pyrrol-1-yl)benzamide | CAS: | 920650-00-6 | MF: | C22H23N3O5S | MW: | 441.5 | EINECS: | | Product Categories: | | Mol File: | 920650-00-6.mol | ![Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- Structure](CAS/20210305/GIF/920650-00-6.gif) |
| Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- Chemical Properties |
density | 1.34±0.1 g/cm3(Predicted) | form | Solid | pka | 11.78±0.70(Predicted) | color | White to off-white |
| Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- Usage And Synthesis |
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]. ?
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 |
| Benzamide, N-[4-methoxy-3-(4-morpholinylsulfonyl)phenyl]-3-(1H-pyrrol-1-yl)- Preparation Products And Raw materials |
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