| Company Name: |
Shanghai Chaolan Chemical Technology Center
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| Tel: |
QQ:65489617 15618227136 |
| Email: |
info@SuperLan-chem.com |
| Products Intro: |
Product Name:WSB1 Degrader 1
CAS:2306039-66-5
Purity:98% Package:5MG;10MG;50MG;100MG,1G,5G,100G
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| Company Name: |
Jingmo (Xiamen) Biotechnology Co., Ltd
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| Tel: |
13621943973 13515979683 |
| Email: |
sales@jamxmpharmatech.com |
| Products Intro: |
Product Name:WSB1 Degrader 1
CAS:2306039-66-5
Purity:>98% Package:1g/;5g/;10g/ Remarks:2g
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| Company Name: |
Bide Pharmatech Ltd.
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| Tel: |
400-1647117 15221909166 |
| Email: |
product02@bidepharm.com |
| Products Intro: |
Product Name:5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine
CAS:2306039-66-5
Purity:98% Package:25mg;50mg;100mg Remarks:BD01404542
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| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:WSB1 Degrader 1;E3 ligating enzyme,oral,inhibit,anticancer,Ubiquitin conjugating enzyme,Ubiquitin activating enzyme,E2 conjugating enzyme,Inhibitor,E1 activating enzyme,E1/E2/E3 Enzyme,WSB1 Degrader 1,metastasis,Ubiquitin ligase,WSB-1 Degrader 1,RhoGDI2,WSB1
CAS:2306039-66-5
Purity:99.64% Package:1 mg;1 mL;10 mg;100 mg;200 mg;25 mg;5 mg;50 mg
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| | 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Basic information |
| Product Name: | 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- | | Synonyms: | 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)-;WSB1 Degrader 1;E3 ligating enzyme,oral,inhibit,anticancer,Ubiquitin conjugating enzyme,Ubiquitin activating enzyme,E2 conjugating enzyme,Inhibitor,E1 activating enzyme,E1/E2/E3 Enzyme,WSB1 Degrader 1,metastasis,Ubiquitin ligase,WSB-1 Degrader 1,RhoGDI2,WSB1;5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine | | CAS: | 2306039-66-5 | | MF: | C21H22N2O2 | | MW: | 334.41 | | EINECS: | | | Product Categories: | | | Mol File: | 2306039-66-5.mol |  |
| | 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Chemical Properties |
| Boiling point | 456.9±45.0 °C(Predicted) | | density | 1.129±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 25 mg/mL (74.76 mM; Need ultrasonic) | | pka | 6.50±0.41(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Usage And Synthesis |
| Biological Activity | WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects[1].
WSB1 Degrader 1 (compound 4; 0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) treatment indues WSB1 degradation in time-dependent and dose-dependent manners[1].WSB1 Degrader 1 (compound 4) exhibits potent antimigration efficacy in both KHOS and H460 cell lines with IC50 values of 39.1 μM and 24.47 μM, respectively[1].WSB1 Degrader 1 (compound 4) significantly inhibits cancer cell migration under normoxia and hypoxia in KHOS cells. WSB1 Degrader 1 (5 μM) treatment elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia[1].The wound-healing of H1299-WSB1 cells is significantly inhibited by treating with WSB1 Degrader 1. WSB1 Degrader 1 can only block the wound-healing capability of wild-type A2780 (A2780-WT) cells but not the A2780-WSB1/KO cells[1].
WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o.; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells[1].In rats, after 100 mg/kg oral dosing or 160 mg/kg intraperitoneal dosing of WSB1 Degrader 1 (compound 4), the two ways of administration are observed with quick absorption (Tmax), but the former dosing displayed a fast clearance (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure[1]. | | References | [1]. Jinxin Che, et al. Discovery of 5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine as a WSB1 Degrader to Inhibit Cancer Cell Metastasis. J Med Chem. 2021 Jun 1. |
| | 2-Pyridinamine, 5,6-bis(4-methoxy-3-methylphenyl)- Preparation Products And Raw materials |
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