货号	规格	价格	上海	北京	珠海	重庆	武汉
S82916-1mg买3赠1	99.80%	￥162.00 S82916-1mg ￥162.00 现货（买3赠1）	8 8	-	-	-	-
S82916-2mg买3赠1	99.80%	￥272.00 S82916-2mg ￥272.00 现货（买3赠1）	9 9	-	-	-	-
S82916-5mg买3赠1	99.80%	￥352.00 S82916-5mg ￥352.00 现货（买3赠1）	5 5	-	-	-	-
S82916-10mg买3赠1	99.80%	￥530.00 S82916-10mg ￥530.00 现货（买3赠1）	2 2	-	-	-	-
S82916-25mg买3赠1	99.80%	￥800.00 S82916-25mg ￥800.00 现货（买3赠1）	4 4	-	-	-	-
S82916-50mg买3赠1	≥98%	￥1490.00 S82916-50mg ￥1490.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S82916-100mg买3赠1	≥98%	￥2720.00 S82916-100mg ￥2720.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.

靶点：

VEGFR2:9.2 nM (IC50);Trk1:0.85 nM (IC50);Trk2:4.6 nM (IC50);Trk3:0.93 nM (IC50);MET:2.7 nM (IC50);TIE2:8 nM (IC50);FLT3:9.3 nM (IC50);VEGFR; Tie-2; FLT; Trkreceptor; c-Met/HGFR

体外研究：

Altiratinib also inhibits MET isoforms METD1228H, METD1228N, METY1230C, METY1230D, METY1230H, METM1250T with IC50s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC50=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC50 of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC50 of 12 nM

体内研究：

A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood–brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases

参考文献：

1. Smith BD, et al. Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated DrugResistance via Balanced Inhibition of MET, TIE2, and VEGFR2. Mol Cancer Ther. 2015 Sep;14(9):2023-34.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.959 ml	9.795 ml	19.59 ml
5 mM	0.392 ml	1.959 ml	3.918 ml
10 mM	0.196 ml	0.98 ml	1.959 ml
50 mM	0.039 ml	0.196 ml	0.392 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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