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首页-小分子抑制剂&激动剂-Tyrosine Kinase-VEGFR-Apatinib
Apatinib

Chemical Structure : Apatinib

CAS No.: 1218779-75-9

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Apatinib (YN 968D1, YN968D1, YN-968D1)

货号: PC-43506Not For Human Use, Lab Use Only.

Apatinib (YN968D1) is a multitargeted tyrosine kinase inhibitor (TKI) that inhibits VEGFR-2 (Flk-1/KDR, IC50=1 nM), RET, c-Kit and c-Src (IC50=13, 429 and 530 nM respectively).

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10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Apatinib (YN968D1) is a multitargeted tyrosine kinase inhibitor (TKI) that inhibits VEGFR-2 (Flk-1/KDR, IC50=1 nM), RET, c-Kit and c-Src (IC50=13, 429 and 530 nM respectively).
Apatinib (YN968D1) significantly increases the accumulation of DOX and Rho 123 in cells overexpressing ABCB1 and ABCG2, inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ, effectively inhibits proliferation, migration and tube formation of HUVECs induced by FBS, and blocks the budding of rat aortic ring.
Apatinib (YN968D1) effectively inhibits the growth of several human tumor xenograft models with little toxicity alone and in combination with chemotherapeutic agents.

物理化学性质&存储条件

分子量 493.58
分子式 C25H27N5O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 32 mg/mL
Chemical Name/SMILES

3-Pyridinecarboxamide, N-[4-(1-cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-, methanesulfonate (1:1)

参考文献

1. Mi YJ, et al. Cancer Res. 2010 Oct 15;70(20):7981-91.

2. Tian S, et al. Cancer Sci. 2011 Jul;102(7):1374-80.

3. Tong XZ, et al. Biochem Pharmacol. 2012 Mar 1;83(5):586-97.

4. Li J, et al. BMC Cancer. 2010 Oct 5;10:529.

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