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Bay 43-9006,Bay43-9006

Sorafenib Tosylate
475207-59-1
315 5mg 起订
730 100mg 起订
上海 更新日期:2023-10-16

爱必信(上海)生物科技有限公司

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产品详情:

中文名称:
Bay 43-9006,Bay43-9006
英文名称:
Sorafenib Tosylate
CAS号:
475207-59-1
保存条件:
store at -20℃ for one year(Powder);
纯度规格:
>98%
产品类别:
激动剂抑制剂

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抑制剂描述:

产品名称:Sorafenib Tosylate

产品别名:对甲苯磺酸索拉非尼

英文别名:Bay 43-9006;Bay43-9006

靶点:Raf-1 ,VEGFR2/Flk1 ,B-Raf ,B-Raf (V599E) ,PDGFRβ

CAS:475207-59-1

 

纯度:>98%

外观:Powder

保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述:

Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

 

溶解性:DMSO127 mg/mL (199.36 mM)

体外研究:

Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib tosylate also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. Sorafenib tosylate weakly inhibits FGFR-1 with IC50 of 580 nM. Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. Sorafenib tosylate markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. Sorafenib tosylate potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. Sorafenib tosylate inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. In addition to inhibition of the RAF/MEK/ERK signaling pathway, Sorafenib tosylate significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. Sorafenib tosylate inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis.

 

体内研究:Oral administration of Sorafenib tosylate (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumor xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumor efficacy, Sorafenib tosylatetreatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumor microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumor xenografts. Sorafenib tosylate treatment produces dose-dependent growth inhibition of PLC/PRF/5 tumor xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumor cell apoptosis.

 

产品信息订购:

  产品货号
  产品名称
  规格
价格
大包装及货期
  abs810719
  Sorafenib Tosylate
  5mg
  300
  立即咨询

产品更多信息请进入爱必信网站咨询

Sorafenib Tosylate; Bay 43-9006;Bay43-9006

公司简介

爱必信(上海)生物科技有限公司成立于2010年,位于上海市申江科创园。是一家自主研发和生产生物试剂的公司。 Absin?是爱必信(上海)生物科技有限公司的试剂品牌,目前已近60万种生化试剂,10万种抗体,其基础生化试剂在基础科学领域得到广泛应用的同时,特色产品线常规生化试剂,血清,小分子激动剂及抑制剂在业界也备受好评。 Absin秉承踏实,务实,求精和不断创新的精神为中国科学家提供最好的产品,努力打造属于中国自己的生物试剂品牌,为广大科学家提供更全面更丰富更优质的产品。 爱科研,必信它(Absin)!Absin努力成为你身边的科研百宝箱!

成立日期 (14年)
注册资本 2500万
员工人数 100-500人
年营业额 ¥ 1000万-5000万
经营模式 工厂
主营行业 生化试剂,抗体,分子生物学,生物活性小分子

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