貨號	規格	價格	上海	北京	武漢	南京
S88568-1mg	99.0%	￥595.00 S88568-1mg ￥595.00 現貨	5 5	-	-	-
S88568-5mg	99.0%	￥1460.00 S88568-5mg ￥1460.00 現貨	7 7	-	-	-
S88568-10mg	99.0%	￥2350.00 S88568-10mg ￥2350.00 現貨	6 6	-	-	-
S88568-25mg	99.0%	￥3900.00 S88568-25mg ￥3900.00 現貨	6 6	-	-	-
S88568-50mg	≥98%	￥5700.00 S88568-50mg ￥5700.00 2-3天	0 貨期：2-3天	-	-	-
S88568-100mg	≥98%	￥7800.00 S88568-100mg ￥7800.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 ?nM and 5.4 nM, respectively.

產品描述：

SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 ?nM and 5.4 nM, respectively.

靶點：

MNK2:5.4 nM (IC50);MNK1:10.8 nM (IC50);MNK

體外研究：

To confirm the kinome selectivity of SLV-2436 (SEL201), the broad KINOMEscan competitive binding assay is performed at 1 μM, which includes 450 distinct kinases. The observed binding profile for SLV-2436 is significantly concentrated in the CAMK family of kinases that comprises MNK1 and MNK2. SLV-2436-treated KIT-mutant melanoma cells have lower oncogenicity and reduced metastatic ability

體內研究：

To investigate the pharmacodynamic properties of SLV-2436 (SEL201), 5 consecutive oral doses of 10, 25, and 50 mg/kg are administered to mice every 12 hours (twice-daily schedule). At the 10 mg/kg twice-daily dosage, 4 hours after the fifth administration, a low plasma concentration of 125 ng/mL SLV-2436 is determined. However, dosing at 25 and 50 mg/kg twice daily, equivalent to 50 and 100 mg/kg/d of SLV-2436, yields substantially increased dose-dependent plasma exposure, reaching an average level of 1,299 ng/mL and 2,075 ng/mL, respectively. At the 24-hour time point, SLV-2436 is still detectable in the plasma, with dose-dependent concentrations of 9, 73, and 124 ng/mL in the 10, 25, and 50 mg/kg twice-daily treatment groups. Oral (p.o.) administration of SLV-2436 at the dosage of 50 mg/kg twice daily, that is, 100 mg/kg/d, for 37 days is well tolerated in mice

參考文獻：

1. Zhan Y, et al. MNK1/2 inhibition limits oncogenicity and metastasis of KIT-mutant melanoma. J Clin Invest. 2017 Nov 1;127(11):4179-4192.

溶解性：

Soluble in DMSO

保存條件：

-20°C

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.851 ml	14.253 ml	28.506 ml
5 mM	0.57 ml	2.851 ml	5.701 ml
10 mM	0.285 ml	1.425 ml	2.851 ml
50 mM	0.057 ml	0.285 ml	0.57 ml

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。

參考文獻

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SLV-2436

SEL201-88; SEL-201