AhR modulator-1

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AhR modulator-1 

AhR modulator-1 (compound 6-MCDF) 是一种选择性的口服活性芳烃受体 (AhR) 调节剂。AhR modulator-1 部分地通过在肿瘤形成之前抑制前列腺 VEGF 的产生而抑制肿瘤转移。AhR modulator-1 在大鼠子宫中也具有抗雌激素特性。

AhR modulator-1

AhR modulator-1 Chemical Structure

CAS No. : 115039-00-4

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生物活性

AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus[1].

IC50 & Target

Aryl hydrocarbon receptor (AhR) [1][2]
Prostatic VEGF[1]
Estrogenic[1]

体外研究
(In Vitro)

AhR modulator-1 (6-MCDF; 0.1-10 μM; 48-96 hours; ASPC-1 cells) treatment exhibits dose-dependent growth inhibitory effects with growth inhibitory effects of 26, 43 and 99% at concentrations of 0.1, 1 and 10 μM, respectively[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: ASPC-1 cells
Concentration: 0.1 μM, 1 μM and 10 μM
Incubation Time: 48 hours, 72 hours, 96 hours
Result: Exhibited dose-dependent growth inhibitory effects.

体内研究
(In Vivo)

AhR modulator-1 (6-MCDF; 0-40 mg/kg; oral administration; daily; for 12 weeks; C57BL/6-Tg(TRAMP)8247Ng/J mice) treatment reduces the frequency of pelvic lymph node metastasis in mice fed the 40 mg/kg diet. And serum VEGF concentrations are also reduced. Prostate tumor incidence and size are not significantly reduced[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6-Tg(TRAMP)8247Ng/J (TRAMP) mice (8-week-old)[1]
Dosage: 0 mg/kg, 10 mg/kg, 40 mg/kg
Administration: Oral administration; daily; for 12 weeks
Result: The frequency of pelvic lymph node metastasis was reduced 5-fold in mice fed the 40 mg /kg diet.S erum VEGF concentrations were also reduced.

分子量

285.55

Formula

C13H7Cl3O

CAS 号

115039-00-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Fritz WA, et al. The selective aryl hydrocarbon receptor modulator 6-methyl-1,3,8-trichlorodibenzofuran inhibits prostate tumor metastasis in TRAMP mice. Biochem Pharmacol. 2009 Apr 1;77(7):1151-60.

    [2]. Koliopanos A, et al. Increased arylhydrocarbon receptor expression offers a potential therapeutic target for pancreatic cancer. Oncogene. 2002 Sep 5;21(39):6059-70.

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