一、产品概述
索拉非尼;Bay 43-9006 是来自Absin品牌的高品质产品，适用于科研实验领域。
更多产品描述请查看优宁维旗下爱必信官网(https://www.absin.cn/sorafenib/abs817880.html?mk_channel=chemicalbook)
二、产品信息
| 货号 | abs817880 |
| SKU货号 | abs817880-10mg |
| 品牌 | Absin |
| 中文名称 | 索拉非尼;Bay 43-9006 |
| 英文名称 | Sorafenib |
| CAS号 | 284461-73-0 |
| 纯度 | ＞98% |
| 分子量 | 464.82 |
| 可溶性 | DMSO : 59 mg/mL (126.9 mM) |
| 外观 | 白色或类白色粉末 |
| 抗原名称 | B-Raf,B-Raf (V599E), Raf-1, VEGFR2/Flk1, VEGFR3, |
商品描述
Sorafenib是Raf-1, B-Raf和VEGFR-2等的多重激酶抑制剂，IC50分别为6 nM, 22 nM和90 nM。
In vitro(体外研究)
Sorafenib inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib 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 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 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 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 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 significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. Sorafenib 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.
In vivo(体内研究)
Oral administration of Sorafenib (~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 treatment 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 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. Sorafenib sensitizes bax-/- cells to TRAIL in a dose-dependent manner, through a mechanism involving down-regulating NF-κB mediated Mcl-1 and cIAP2 expression. Combining Sorafenib (30-60 mg/kg) with TRAIL (5 mg/kg) show dramatic efficacy in TRAIL-resistant HCT116 bax-/- and HT29 tumor xenografts.
三、背景
| 别名 | 索拉非尼；Bay 43-9006 |
| CAS号 | 284461-73-0 |
四、制备和贮存
| 保存方式 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
五、产品特点
- 品质保证：经过严格的质量控制，确保产品的高品质和稳定性。
- 高纯度：纯度达到<p>＞98%</p>。
六、注意事项
- 本产品仅供科学研究使用，不可用于临床诊断或治疗。
- 请在通风良好的环境下操作，佩戴适当的个人防护装备。
- 如不慎接触皮肤或眼睛，请立即用大量清水冲洗并就医。