AZ12672857

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZ12672857 是 EphB4 的抑制剂，IC50 为 1.3 nM。 AZ12672857 抑制 Src 转染的 3T3 细胞的细胞增殖，IC50 为 2 nM，并抑制转染的 CHO-K1 细胞中 EphB4 的自磷酸化，IC50 为 9 nM。

AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.(In Vitro):AZ12672857 shows IC50s of 240 nM and 58 nM for p-KDR in HUVEC and p-PDGFR-β in MG63 cell line. AZ12672857 moderately inhibits CYP P450 with IC50s of 5 μM for 2C9 and 3A4 and >10 μM for 1A4, 2D6 and 2C19.

AZ12672857 shows only modest inhibition of CYP P450 (IC50=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC50 of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC50 of 58 nM.

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Angiogenesis

Src

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945396-55-4

486.57

C26H30N8O2

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (51.38 mM)

N1=CC=2C(=CC=CC2N(C3=NC(=NC=C3)NC=4C=C(C=C(C4)N5CCOCC5)N6CCOCC6)C)N1

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(-20℃)

With Ice Pack

≥ 2 years