SI-2 hydrochloride

Research use only, not for human use.

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.

SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.

Cell Viability Assay.Cell Line:MDA-MB-468 cells.Concentration:100 nM.Incubation Time:12 hours.Result:Significantly reduced the motility of cancer cells.Western Blot Analysis.Cell Line:MDAMB-468 cells. Concentration:0-200 nM.Incubation Time:24 hours.Result:Significantly reduced SRC-3 protein levels. Did not decrease the SRC-3 mRNA level.Western Blot Analysis.Cell Line:Cancer cells.Concentration:0-200 nM.Incubation Time:24 hours. Result:Caused PARP cleavage.

Animal Model:MDA-MB-468 breast cancer mouse model.Dosage:2 mg/kg.Administration:Twice daily for 5 weeks (Vehicle, PBS).Result:Significantly inhibit tumor growth.SRC-3 levels in SI-2–treated tumor tissues were significantly lower than the PBS treated control group.Animal Model:CD1 mice.Dosage:20 mg/kg (Pharmacokinetic Analysis).Administration:Intraperitoneal administration once.Result:T1/2 = 1 h, Cmax of 3.0 μM, and the time to reach the maximum plasma concentration tmax of 0.25 h.SI-2 only degrades slightly (less than 5%) at pH 1.6 and 3.0 within 6 h, and is stable in buffers with pH ≥ 5.

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Angiogenesis

Src

Src

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1992052-49-9

301.77

C15H16ClN5

>98% (HPLC)

In Vitro:?DMSO : 5 mg/mL (16.57 mM; Ultrasonic )

Cl.C\C(=N/Nc1nc2ccccc2n1C)c1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years