| Company Name: |
Tianjin Kailiqi Biotechnology Co., Ltd.
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| Tel: |
15076683720 |
| Email: |
klq@cw-bio.com |
| Products Intro: |
Product Name:STAT3-IN-17
CAS:1245814-52-1
Purity:大于98% Package:1g,5g,10g,25g根据客户需要分装 Remarks:Not For Human Use, Lab Use Only.
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| Company Name: |
ChemeGen
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| Tel: |
18818260767 |
| Email: |
2625930290@qq.com |
| Products Intro: |
Product Name:CAY10784
CAS:1245814-52-1
Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| | CAY10784 Basic information |
| Product Name: | CAY10784 | | Synonyms: | CAY10784;CAY10784,CAY-10784;Benzamide, N-(5-nitro-2-thiazolyl)-4-(trifluoromethyl)-;N-(5-nitro-2-thiazolyl)-4-(trifluoromethyl)-benzamide;STAT3-IN-17;N-(5-Nitrothiazol-2-yl)-4-(trifluoromethyl)benzamide | | CAS: | 1245814-52-1 | | MF: | C11H6F3N3O3S | | MW: | 317.24 | | EINECS: | | | Product Categories: | | | Mol File: | 1245814-52-1.mol |  |
| | CAY10784 Chemical Properties |
| density | 1.615±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml,DMSO: 10 mg/ml,Ethanol: 1 mg/ml | | form | A crystalline solid | | pka | 5.82±0.50(Predicted) | | color | Light yellow to yellow |
| | CAY10784 Usage And Synthesis |
| Uses | STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori[1][2]. | | Biological Activity | CAY10784 is a STAT3 inhibitor (IC50 = 0.74 μM in a reporter assay) and a derivative of WP1066 .1 It inhibits proliferation of HeLa, Caco-2, A549, A375, U87MG, and HL-60 cancer cells (IC50s = 1.8, 1.8, 3, 2.8, 2.3, and 1.2 μM, respectively) but not PC3 or HT-29 cancer cells (IC50s = >10 μM for both). CAY10784 is also active against H. pylori and C. jejuni (MICs = 1.6 and 4.7 μM, respectively).2 | | in vivo | STAT3-IN-17 (compound 15) (5 mg/kg for ig, or 25 mg/kg for iv; single dose) exhibits greater pharmacokinetic properties than Nitazoxanide (HY-B0217) in rat, with a significantly longer half-life for elimination (t1/2β) (11.1 vs 0.8 h), greater absolute bioavailability (F) (87.4% vs 5.7%), and higher maximum plasma concentration (Cmax) (20.7 vs 1.0 mg/L) maximum plasma concentration (Cmax) (20.7 vs 1.0 mg/L)[1].
| | IC 50 | STAT3 | | References | 1.Lü, Z., Li, X., Li, K., et al.Structure-activity study of nitazoxanide derivatives as novel STAT3 pathway inhibitorsACS Med. Chem. Lett.(2021)
2.Ballard, T.E., Wang, X., Olekhnovich, I., et al.Synthesis and antimicrobial evaluation of nitazoxanide-based analogues: Identification of selective and broad spectrum activityChemMedChem6(2)362-377(2011) |
| | CAY10784 Preparation Products And Raw materials |
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