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產品描述： LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases |
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靶點：
TDO;Others |
體內研究：
LM10 (160 mg/kg; p.o.) prevents the growth of TDO-expressing P815 tumor cells and promotes better rejection of control clone P815B cl1, which does not express TDO. LM10 displays a good TDO inhibition (Ki = 5.6 μM) with a competitive inhibition profile. LM10 does not inhibit IDO and has a high solubility and bioavailability without obvious signs of toxicity. The plasma concentration of LM10 after oral administration of 160 mg/kg/day is between 20 and 40 μg/mL (87-175 μM), a concentration about 40 times above the IC50 measured in the cellular assay performed with the physiological concentration of plasma tryptophan. |
參考文獻：
1. Pilotte L, et al. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase. Proc Natl Acad Sci U S A. 2012;109(7):2497-2502. |
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溶解性：
DMSO : 50 mg/mL (218.14 mM; Need ultrasonic) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
4.363 ml |
21.814 ml |
43.628 ml |
| 5 mM |
0.873 ml |
4.363 ml |
8.726 ml |
| 10 mM |
0.436 ml |
2.181 ml |
4.363 ml |
| 50 mM |
0.087 ml |
0.436 ml |
0.873 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京