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IDO-IN-1

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Chemical Structure| 914638-30-5 同义名 : -
CAS号 : 914638-30-5
货号 : A401416
分子式 : C9H7BrFN5O2
纯度 : 98+%
分子量 : 316.087
MDL号 : MFCD28399146
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 115 mg/mL(363.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Indoleamine 2,3-dioxygenase (IDO) is one of the key heme-containing dioxygenases that catalyze the rate limiting step in the catabolism of the essential amino acid tryptophan to N-formylkynurenine by oxidative cleavage of the indole 2,3 double bond[2]. IDO-IN-1 is an IDO inhibitor with IC50 of 59 nM[3]. C57BL/6 mice bearing GMCSF-secreting B16 tumors were subcutaneously administered with IDO-IN-1 at 25, 50, and 75 mg/kg b.i.d. and 50% tumor growth inhibition was observed at 75 mg/kg[3].
作用机制 IDO-IN-1 bounds to IDO through the oxygen of the hydroxyamidine to the iron of the heme in the ferrous state.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.82mL

3.16mL

1.58mL

31.64mL

6.33mL

3.16mL
参考文献

[1]Yue EW, et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7.

[2]Munn DH, Mellor AL. Indoleamine 2,3-dioxygenase and tumor-induced tolerance. J Clin Invest. 2007 May;117(5):1147-54. doi: 10.1172/JCI31178. PMID: 17476344; PMCID: PMC1857253.

[3]Yue EW, Douty B, Wayland B, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Liu C, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Metcalf B, Scherle PA, Combs AP. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J Med Chem. 2009 Dec 10;52(23):7364-7. doi: 10.1021/jm900518f. PMID: 19507862.