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抑制剂/激活剂

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凋亡与自噬

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RO4929097

RO4929097 (RG-4733)是一种γ secretase抑制剂，无细胞试验中IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。Phase 2。

货号：
TK0465
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	847925-91-1
生物活性	RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
分子式	C22H20F5N3O3
分子量	469.4
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, stored under nitrogen,*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据	DMSO : ≥ 49 mg/mL (104.39 mM)
体内研究	RO4929097 (3-60 mg/kg, p.o.) results in significant tumor growth inhibition in nude mice bearing A549 NSCLC xenografts, compared with vehicle-treated animals. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially causes regression of established A549 tumors. RO4929097 impairs the growth of primary melanoma cells in vivo. The percentage of secondary tumors formed by RO4929097-treated cells is lower; the secondary tumors formed by RO4929097-treated cells are smaller; a significant delay in tumor formation by the RO4929097-treated cells compared to the vehicle-treated ones is observed in mice injected with 10 cells in vivo.
体外研究	RO4929097 inhibits the production of ICN reducing the expression of the downstream Notch target, Hes1, producing a less transformed morphology in A549 cells. RO4929097 inhibits Notch processing in human tumor-derived cells. RO4929097 (1 µM) inhibits the growth of breast cancer cells, and the inhibition is 20% for SUM149 and 10% for SUM190 cells. RO4929097 does not have a marked effect in invasiveness of SUM149 cells. RO4929097 significantly reduces colony formation by both cell lines with the effect being more notable in SUM149 than by SUM190 cells. RO4929097 inhibits proliferation, anchorage independent growth, and sphere formation of primary melanoma cells in vitro.
纯度及产品资料	98%

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