Saracatinib

Research use only, not for human use.

A potent, highly selective, orally available, dual Src/Abl kinase inhibitor with IC50 of 2.7, 4, 4 and 30 nM for c-Src, Yes, Lck and Abl, respectively.

A potent, highly selective, orally available, dual Src/Abl kinase inhibitor with IC50 of 2.7, 4, 4 and 30 nM for c-Src, Yes, Lck and Abl, respectively; displays high selectivity over a range of kinases (Csk, VEGFR-2, Flt-4, EGFR, and PDGFR); exhibits potent inhibition of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo.Breast Cancer Phase 2 Clinical(In Vitro):Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC50 of 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC50 values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC50 of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC50 0.14 μM).(In Vivo):Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats).

Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC50 of 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC50 values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC50 of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC50 0.14 μM).

Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats).

AZD0530 | AZD-0530 | AZD 0530

Angiogenesis

Src

BLK|c-Kit|c-Src|c-Yes|EGFR|EGFR(L858R)|EGFR(L861Q)|EphA2|FGR|Fyn|Lck|Lyn|v-Abl|EGFRL861Q|EGFRL858R

Cancer

Breast Cancer

379231-04-6

542.0265

C27H32ClN5O5

>98% (HPLC)

DMSO: ≥ 32 mg/mL

CN1CCN(CCOC2=CC3=NC=NC(NC4=C5OCOC5=CC=C4Cl)=C3C(OC6CCOCC6)=C2)CC1

4-Quinazolinamine, N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-

(-20℃)

With Ice Pack

≥ 2 years