货号	规格	价格	上海	北京	珠海	重庆	武汉
S89207-5mg促销	99.80%	￥1500.00 ￥1200.00 S89207-5mg ￥1200.00 现货	5 5	-	-	-	-
S89207-10mg促销	99.80%	￥2400.00 ￥1920.00 S89207-10mg ￥1920.00 现货	6 6	-	-	-	-
S89207-25mg促销	99.80%	￥4500.00 ￥3600.00 S89207-25mg ￥3600.00 现货	4 4	-	-	-	-
S89207-100mg促销	≥98%	￥9790.00 ￥7830.00 S89207-100mg ￥7830.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity

靶点：

FGFR1:31.1 nM (IC50);DDR2:3.2 nM (IC50)

体外研究：

FGFR1/DDR2 inhibitor 1 (compound 11k) (25-200 μM; 2 hours) shows significant inhibition of FGFR2 phosphorylation in a dose-dependent manner in SNU16 cells. FGFR1/DDR2 inhibitor 1 shows (60-250 μM; 2 hours) significant inhibition of DDR2 phosphorylation in a dose-dependent manner in H2286 cells. FGFR1/DDR2 inhibitor 1 significantly inhibits the proliferation of FGFR-driven cancer cell lines with IC50s of 108.4, 93.4, 31.8 and 306.6 nM against KG-1, SNU-16, NCI-H716 and UMUC14 respectively. FGFR1/DDR2 inhibitor 1 demonstrates substantially activity against the DDR2-driven cancer cell line NCI-H2286 (93.0 nM)

体内研究：

FGFR1/DDR2 inhibitor 1 (10-20 mg/kg; p.o.; once daily for 7 days) has profound anti-tumor efficacy in NCI-H1581 tumor model. SCID mice bearing NCI-H2286 tumors were randomized and treated with FGFR1/DDR2 inhibitor 1 at doses of 10 mg/kg for 10 consecutive days. FGFR1/DDR2 inhibitor 1 could suppress tumor growth with tumor growth inhibition rates (TGI) of 82.8%. Animal Model: Nude mice bearing NCI-H1581 tumors Dosage: 10 or 20 mg/kg Administration: P.o.; once daily for 7 days Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition rates (TGI) of 59.7% and 98.1% at doses of 10 and 20 mg/kg, respectively.

参考文献：

1. Wang Q, et al. Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma. Eur J Med Chem. 2019 Feb 1;163:671-689.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.994 ml	9.97 ml	19.94 ml
5 mM	0.399 ml	1.994 ml	3.988 ml
10 mM	0.199 ml	0.997 ml	1.994 ml
50 mM	0.04 ml	0.199 ml	0.399 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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