貨號	規格	價格	上海	北京	武漢	南京
S88571-5mg	≥98%	￥2500.00 S88571-5mg ￥2500.00 2-3天	0 貨期：2-3天	-	-	-
S88571-10mg	≥98%	￥3800.00 S88571-10mg ￥3800.00 2-3天	0 貨期：2-3天	-	-	-
S88571-25mg	≥98%	￥6900.00 S88571-25mg ￥6900.00 2-3天	0 貨期：2-3天	-	-	-
S88571-50mg	≥98%	￥9900.00 S88571-50mg ￥9900.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

產品描述：

Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

靶點：

ERK2:0.6 nM (IC50);ERK

體外研究：

Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib

體內研究：

Tumor growth inhibition by Tizaterkib ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and Tizaterkib ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and Tizaterkib ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and Tizaterkib ethanesulfonic acid results in a reduction in tumor growth

參考文獻：

1. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

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	2.022 ml	10.111 ml	20.222 ml
5 mM	0.404 ml	2.022 ml	4.044 ml
10 mM	0.202 ml	1.011 ml	2.022 ml
50 mM	0.04 ml	0.202 ml	0.404 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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CS-2696

AZD0364