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99%min Dabrafenib Manufacturer For Melanoma Drugs CAS NO.1195765-45-7
- Min.Order: 10 Gram
- Payment Terms: T/T,
- Product Details
Keywords
- N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide Basic information
- Dabrafenib Manufacturer
- For Anticancer
Quick Details
- ProName: 99%min Dabrafenib Manufacturer For Mel...
- CasNo: 1195765-45-7
- Molecular Formula: C23H20F3N5O2S2
- Appearance: White Powder
- Application: It Can Be Used As Pharmaceutical Inte...
- DeliveryTime: 2-4 days after confirming your payment...
- PackAge: 100g/ bag, 2 kg/ bag, 25kg/ carton or ...
- Port: Wuhan
- ProductionCapacity: 10000 Metric Ton/Month
- Purity: 99%
- Storage: Store in sealed containers at cool & d...
- Transportation: By DHL, TNT, FedEx, HKEMS, UPS, Etc
- LimitNum: 10 Gram
Superiority
Advantages:
Hubei XinRunde Chemical Co., Ltd is a renowned pharmaceutical manufacturer. We can offer high quality products at competitive price in quick delivery with 100% custom pass guaranteed. Never stop striving to offer our best service is our philosophy. We have Flexible and Untraceable payment terms. As a leading manufacture, our products have been exported to Germany, Norway, Poland, Finland, Spain, UK, France, Russia, USA, Brazil, Mexico, Australia, Japan, Korea, Thailand, Indonesia, Uruguay and many other countries.
1. Quality.Every batch of steroid powders have tobetested by our QC(quality control) before they are allowed to sell.
2. Delivery We have stock, so we can delivery quickly at the very day when receive the payment. Within 24 hours after receiving the payment Lead time 4 or 7 days.
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Details
| N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide Basic information |
| Product Name: | N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide |
| Synonyms: | Dabrafenib;N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide;Dabrafenib free base(GSK2118436A);Dabrafenib (GSK2118436);GSK2118436A;Dabrafenib (GSK2118436A);Dabrafenib KB-57246;Debrafenib API |
| CAS: | 1195765-45-7 |
| MF: | C23H20F3N5O2S2 |
| MW: | 519.5624096 |
| EINECS: | 1592732-453-0 |
| Product Categories: | Raf B protein kinase inhibitor;inhibitor;MAPK;Inhibitors |
| Mol File: | 1195765-45-7.mol |
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| N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide Chemical Properties |
| density | 1.443 |
| Safety Information |
| N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide Usage And Synthesis |
| Overview |
Dabrafenib(trade name Tafinlar, GSK2118436) is a type of targeted therapy known as a signal transduction inhibitor that helps slow or stop the growth and spread of melanoma cells in the form of methanesulfonate for medicinal purposes. Trametinib was previously approved in 2013 as a single agent for treatment of BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma. Dabrafenib was also approved in 2013 as a single agent for treatment of BRAF V600E mutation-positive unresectable or metastatic melanoma. Trametinib and dabrafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. The combination of these two drugs is considered to be able to produce more effective and lasting therapeutical effect of melanoma, and the composition of two drugs are also considered to be major business opportunities of two drugs. The patients who have advanced stages of melanoma will benifit from this drug: Stage III that is unresectable (unable to be completely removed by surgery) Stage IV, also known as metastatic (melanoma cells that have spread to organs and other parts of the body). If you have advanced melanoma, your physician will test you for BRAF mutations before prescribing dabrafenib. The physician will send a biopsy (sample of cancer tissue removed from your body) to a special lab for analysis. Dabrafenib: When given by itself, works only in patients who have tested positive for the BRAF V600E mutation. Cannot be used to treat patients with the wild-type BRAF mutation. |
| Synthetic Methods |
The key step in the synthesis of Dabrafenib is the construction of the 1,3-thiazole ring, which is usually carried out by the closing ring directly of thioamide (as a 1,3-binuclear reagent) and anα-carbonyl halide (as a 1,2-amphiphilic reagent). Sulfonyl chloride 1 and aniline 2 gave sulfonamide 3 under basic conditions. Methyl pyrimidine 4 with non-nucleophilic strong alkali LiHMDS pull out the acid proton on the methyl and react with 3 to obtain 5, and the latter has α-bromination with NBS to obtain 1,2-amphiphilic reagent 6, and then 6 reacts with 1 , 3-parent nucleotides 7 to close the ring to obtain 8, and finally reacts with ammonia to obtain Dabrafenib. Figure 1: synthetic route of Dabrafenib |
| Biological activity | Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with an IC50 of 0.8 nM, and effects for B-Raf (wt) and c-Raf is 4 and 6 fold lower respectively. |
| How to use |
It is usually taken twice a day on an empty stomach, 1 hour before or 2 hours after a meal. Take dabrafenib about 12 hours apart at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Do not stop taking dabrafenib without talking to your doctor. Swallow the capsules whole; do not split, chew, or crush them. Your doctor may adjust your dose of dabrafenib depending on your response to treatment and any side effects that you experience. Talk to your doctor about how you are feeling during your treatment. |
| Major Side Effects |
The following side effects are common (occurring in greater than 30%) for patients taking dabrafenib :
These side effects are less common side effects (occurring in about 10-29%) of patients receiving dabrafenib:
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| In vitro | Dabrafenib is selective for Raf kinases and is 400 times more active against B-Raf than other tested 91% kinases. Dabrafenib inhibits B-RafV600E kinase, resulting in reduced phosphorylation of ERK and inhibition of cell proliferation. The cells stagnate in the G1 phase in cancer cells that specifically encode mutated B-RafV600E. |
| In vivo | Dabrafenib (oral) inhibits the growth of B-RafV600E mutated melanoma (A375P). Dabrafenib (oral) also inhibits tumor growth, subcutaneously injecting colon cancer (Colo205) in immunocompromised mice. |
| Definition | ChEBI: An organofluorine compound and antineoplastic agent, used as its mesylate salt in treatment of metastatic melanoma. |
