SI-2 hydrochloride

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

SI-2 (EPH 116 hydrochloride) 是 SRC-3 的抑制剂，诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 (EPH 116 hydrochloride) 具有良好的药代动力学特征和改善的毒性，以及可接受的口服可用性。

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.

——

Angiogenesis

Src

Src

——

——

1992052-49-9

301.77

C15H16ClN5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 5 mg/mL (16.57 mM; 超声助溶 )

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

——

(-20℃)

With Ice Pack

≥ 2 years