AT9283

AT9283

Biochem/physiol Actions

AT9283 has also been shown to accelerate growth arrest in various xenograft models.

AT9283 is an ATP site-targeting pyrazole-benzimidazole-based molecule with inhibitory potency against multiple kinases, most notably Aurora A/B (IC50 ≤3.0 nM), JAK2/3 (IC50 = 1.2/1.1 nM), Abl T315I (IC50 = 4 nM), GSK3β, FGFR2, VEGFR3 (Flt4), Mer, Ret, Rsk2/3, Tyk2, Yes (IC50 = 1-10 nM). AT9283 also inhibits 72 other kinases/mutations at a reduced potency (IC50 = 10-30 nM against 14, 30-100 nM against 21, 100-300 against 37 targets), while displaying an IC50 >300 nM toward 144 other kinase targets. AT9283 inhibits the growth/survival of multiple solid tumor cell lines in vitro (IC50 = 7.7-20 nM) and shows anti-cancer efficacy in mice via i.p. injection in vivo (67% and 76%HCT116 tumor growth inhibition on day 16, respectively, with 15 and 20 mg/kg b.i.d., two-day on and two-day off; >95% inhibition of Ba/F3 ETV6-JAK2 leukemia proliferation on day 12 with 10 mg/kg b.i.d. on days 2–5 and 8–12).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576253 AT9283 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£334.29 (exc VAT) per 25MG
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3576254 AT9283 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£104.05 (exc VAT) per 5MG
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