Company Name: |
TargetMol Chemicals Inc.
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Tel: |
4008200310 |
Email: |
marketing@tsbiochem.com |
Products Intro: |
Product Name:TNIK-IN-3;TNIK IN 3,TNIKIN3 CAS:2754265-25-1 Purity:99.56% Package:1 mg;1 mL;10 mg;100 mg;25 mg;5 mg;50 mg
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Company Name: |
Nanjing Tengyi Biotechnology Co., Ltd
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Tel: |
025-58851786 17714337195 |
Email: |
sales@tybiochem.com |
Products Intro: |
Product Name:1,4-Benzoxazepin-5(2H)-one, 4-[(4-fluorophenyl)methyl]-3,4-dihydro-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)- CAS:2754265-25-1 Purity:95+% Package:1g;5g
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Company Name: |
https://hanhongsci.com/
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Tel: |
021-54306202 18917919676 |
Email: |
info@hanhongsci.com |
Products Intro: |
Product Name:TNIK-IN-3 CAS:2754265-25-1 Purity:99.88% Package:5mg;25mg;100mg;1g;5g
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Company Name: |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
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Tel: |
021-59167510 18117107507 |
Email: |
vip@med-life.cn |
Products Intro: |
Product Name:TNIK-IN-3 CAS:2754265-25-1 Purity:>=99% Package:10mM*1mLinDMSO;10mg;50mg;5mg;100mg;25mg
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| 1,4-Benzoxazepin-5(2H)-one, 4-[(4-fluorophenyl)methyl]-3,4-dihydro-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)- Basic information |
| 1,4-Benzoxazepin-5(2H)-one, 4-[(4-fluorophenyl)methyl]-3,4-dihydro-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)- Chemical Properties |
density | 1.354±0.06 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | DMSO : 83.33 mg/mL (215.10 mM; Need ultrasonic) | pka | 13.48±0.40(Predicted) | form | Solid | color | Off-white to light yellow |
| 1,4-Benzoxazepin-5(2H)-one, 4-[(4-fluorophenyl)methyl]-3,4-dihydro-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)- Usage And Synthesis |
Biological Activity | TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer[1].
TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC50s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively[1].TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC50s of 4.26 μM and 8.00 μM, respectively[1].TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells[1].TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells[1].TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells[1].TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells[1].
TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner[1]. | References | [1]. Li Y, et, al. Discovery of 3,4-Dihydrobenzo[ f][1,4]oxazepin-5(2 H)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects. J Med Chem. 2022 Jan 5. |
| 1,4-Benzoxazepin-5(2H)-one, 4-[(4-fluorophenyl)methyl]-3,4-dihydro-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)- Preparation Products And Raw materials |
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