Sorafenib-d3 tosylate
Based on 1 publication(s) in Google Scholar
Sorafenib-d3 (Donafenib) tosylate is the deuterated-labeled Sorafenib tosylate (HY-10201A). Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 1333386-17-6
- Formula: C28H21D3ClF3N4O6S
- Molecular Weight:640.05
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Sorafenib-d3 tosylate
MoreAll VEGFR Isoforms
MoreAll MEK Isoforms
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Biological Activity
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VEGFR3 20 nM (IC50) |
Braf 22 nM (IC50) |
Raf-1 6 nM (IC50) |
VEGFR2 15 nM (IC50) |
BrafV599E 38 nM (IC50) |
STAT3 |
MMP-2 |
Bcl-xL |
Bcl-2 |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1333386-17-6
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Unlabeled Cas 475207-59-1
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Molecular Weight 640.05
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Formula C28H21D3ClF3N4O6S
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SMILES
O=S(O)(C1=CC=C(C=C1)C)=O.[2H]C([2H])([2H])NC(C2=CC(OC3=CC=C(C=C3)NC(NC4=CC(C(F)(F)F)=C(C=C4)Cl)=O)=CC=N2)=O
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Synonyms
Donafenib tosylate; Bay 43-9006-d3 tosylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Purity & Documentation
References
[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. [Content Brief]
[2]. Heim M, et al. The Raf kinase inhibitor BAY 43-9006 reduces cellular uptake of platinum compounds and cytotoxicity in human colorectal carcinoma cell lines. Anticancer Drugs. 2005;16(2):129-136. [Content Brief]
[3]. Gu FM, et al. Sorafenib inhibits growth and metastasis of hepatocellular carcinoma by blocking STAT3. World J Gastroenterol. 2011 Sep 14;17(34):3922-32. [Content Brief]
[4]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. [Content Brief]
[5]. Li M, et al. Activation of an AKT/FOXM1/STMN1 pathway drives resistance to tyrosine kinase inhibitors in lung cancer. Br J Cancer. 2017;117(7):974-983. [Content Brief]
[6]. Jin W, et al. Long non-coding RNA TUC338 is functionally involved in sorafenib-sensitized hepatocarcinoma cells by targeting RASAL1. Oncol Rep. 2017;37(1):273-280. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sorafenib-d3 tosylate Related Classifications
HY-10201S4 Related Classifications
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