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印度sorafenib

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-03-27 09:59:04

【药品简介】 多吉美sorafenib(索拉非尼片),适应症为 1.治疗不能手术的晚期肾细胞癌。2.治疗无法手术或远处转移的肝细胞癌。

【适应症状】 sorafenib,处方药。无法手术切除的肝细胞肝癌;晚期肾癌;局部复发或转移的、进展性、放射性碘难治型分化型甲状腺癌

【 药品别名 】 多吉美 索拉非尼

印度sorafenib(多吉美 索拉非尼)价格,正品图片,治疗肝癌药物, 购买sorafenib请到印度药房官方网站进行购买 【印度药房大全目录】

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【印度sorafenib说明书,怎么吃?】

【sorafenib作用机制】   

多激酶抑制剂,通过抑制细胞内Raf激酶(CRAF,BRAF,突变的BRAF)和细胞表面激酶受体(VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-beta, cKIT, FLT-3, RET, RET/PTC),达到抑制肿瘤生长和新生血管形成。
 
【副作用】 

乏力、恶心、呕吐、腹泻、便秘、皮肤干燥、脱发、头痛等

【参考用法】
 
肝癌:口服,400mg 每天两次,直至疾病进展或不可接受的毒性

晚期肾癌:口服,400mg 每天两次,直至疾病进展或不可接受的毒性

甲状腺癌,分化型:口服,400mg 每天两次,直至疾病进展或不可接受的毒性

【注意事项】

对疑似不良反应的处理包括暂停或减少索拉非尼用量,如必需,索拉非尼的用量减为每日一次或隔日一次,每次0.4g(2×0.2g)


USES OF SORANIB TABLET
Liver cancer
Kidney cancer
Thyroid cancer

SORANIB TABLET SIDE EFFECTS
Common
Fatigue
Nausea
Loss of appetite
Diarrhea
Abdominal pain
Hair loss
Weight loss
Rash
Painful blisters on hands and feet

HOW TO USE SORANIB TABLET
Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Soranib Tablet is to be taken empty stomach.
Avoid Soranib Tablet with high-fat meals such as olive oil, nuts & seeds (Brazil nuts), dark chocolate, butter and meat.

HOW SORANIB TABLET WORKS
Soranib Tablet is an anti-cancer medication. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps to stop or slow the spread of cancer cells.

SORANIB TABLET RELATED WARNINGS
warnings
Alcohol
Interaction with alcohol is unknown. Please consult your doctor.
warnings
Pregnancy

WEIGH RISKS VS BENEFITS
Soranib Tablet is unsafe to use during pregnancy.
There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk, for example in life-threatening situations. Please consult your doctor.

warnings
Lactation
Soranib Tablet is probably safe to use during lactation. Limited human data suggests that the drug does not represent a significant risk to the baby.

warnings
Driving
SAFE
Soranib Tablet does not usually affect your ability to drive.

warnings
Kidney
SAFE
Soranib Tablet is safe to use in patients with kidney disease. No dose adjustment of Soranib Tablet is recommended.
Regular monitoring of blood tests may be advised while you are taking this medicine.

warnings
Liver
Soranib Tablet should be used with caution in patients with severe liver disease. Dose adjustment of Soranib Tablet may be needed. Please consult your doctor.
WHAT IF YOU MISS A DOSE OF SORANIB TABLET?
If you miss a dose of Soranib Tablet, skip it and continue with your normal schedule. Do not double the dose.

Sorafenib

生物活性

产品描述

Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).

靶点活性

B-Raf,22nM

B-Raf (V599E),38nM

Raf-1,6nM

VEGFR2/Flk1,15nM

VEGFR3,20nM

体外活性

Sorafenib tosylate明显抑制NIH 3T3细胞中VEGFR2磷酸化和HEK-293细胞中Flt-3磷酸化。Sorafenib tosylate也能有效抑制mVEGFR2 (Flk-1),mVEGFR3,mPDGFRβ,Flt3和c-Kit,IC50分别为15 nM,20 nM,57 nM,58 nM和68 nM。Sorafenib tosylate抑制野生型和V599E突变型B-Raf活性,IC50分别为22 nM和38 nM。Sorafenib tosylate抑制HAoSMC和MDA-MB-231细胞的增殖,IC50分别为0.28 μM和2.6 μM。Sorafenib tosylate除了抑制RAF/MEK/ERK信号通路,明显抑制eIF4E的磷酸化作用,并以MEK/ERK依赖的方式降低肝癌的细胞中Mcl-1水平。Sorafenib tosylate抑制PLC/PRF/5和HepG2细胞的增殖,IC50分别为6.3 μM和4.5 μM,并诱导细胞凋亡。

体内活性

30-60 mg/kg Sorafenib与5 mg/kg TRAIL结合对TRAIL抗性HCT116 bax-/-和HT29肿瘤异种移植物有明显的功效。口服60 mg/kg Sorafenib tosylate ,对人肿瘤异种移植模MDA-MB-231,Colo-205,HT-29,DLD-1,NCI-H460和A549表现出广谱的、剂量依赖性抗肿瘤活性,并且没有毒性。Sorafenib通过下调NF-κB介导的Mcl-1 和 cIAP2的表达使bax-/-细胞对TRAIL剂量依赖性敏感。Sorafenib tosylate有效抑制HT-29 和 MDA-MB-231异种移植物中MEK 1/2磷酸化和pERK 1/2水平,并且明显抑制MDA MB-231,HT-29和Colo-205肿瘤异种移植物中肿瘤微血管面积和微血管密度。

激酶实验

Biochemical assays: Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The Raf kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ[33P]ATP (400 Ci/mol) and incubated at 32 °C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labeled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, Sorafenib tosylate is added before the enzyme initiation. A 50-fold stock plate is made with Sorafenib tosylate serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final Sorafenib tosylate concentrations range from 10 μM to 4.56 nM in 1% DMSO.

细胞实验

Cells are exposed to increasing concentrations of Sorafenib tosylate for 72 hours. Cell number is quantitated using the Cell TiterGlo ATP Luminescent assay kit. This assay measures the number of viable cells per well by measurement of luminescent signal based on amount of cellular ATP. (Only for Reference)

细胞系: MDA-MB-231, and HAoSMC

动物实验

动物模型:FeNCr-nu/nu mice implanted s.c. with MDA-MB-231, Colo-205, HT-29, H460, or A549 cells

化学信息

分子量

464.83

分子式

C21H16ClF3N4O3

CAS

284461-73-0

溶解度

DMSO: 59 mg/mL (126.9 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

  1 mg 5 mg 10 mg
1 mM 2.151 ml 10.757 ml 21.513 ml
5 mM 0.43 ml 2.151 ml 4.303 ml
10 mM 0.215 ml 1.076 ml 2.151 ml
50 mM 0.043 ml 0.215 ml 0.43 ml
参考文献
 
1. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109.
2. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83.
3. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16.
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