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Apatinib

Chemical Structure : Apatinib

CAS No.: 1218779-75-9

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

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 493.58
Formula C25H27N5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

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

References

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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