Dabrafenib Mesylate
- CAS No.
- 1195768-06-9
- Chemical Name:
- Dabrafenib Mesylate
- Synonyms
- Dabrafenib Mesylate;GSK 2118436B;Dapafini mesylate;abrafenibmesylate;Dabrfenib Mesylate;GSK2118436 Mesylate;GSK-2118436 Mesylate;GSK 2118436 Mesylate;Debrafenib Mesylate (API);Dabrafenib Mesylate (API)
- CBNumber:
- CB72630077
- Molecular Formula:
- C24H24F3N5O5S3
- Molecular Weight:
- 615.66
- MDL Number:
- MFCD20922872
- MOL File:
- 1195768-06-9.mol
Melting point | >234oC (dec.) |
---|---|
storage temp. | Hygroscopic, -20°C Freezer, Under inert atmosphere |
solubility | DMSO (Slightly, Heated), Methanol (Slightly) |
form | White solid. |
color | White to Off-White |
Stability | Hygroscopic |
InChIKey | YKGMKSIHIVVYKY-UHFFFAOYSA-N |
SMILES | S(O)(=O)(=O)C.FC1C(=CC=CC=1C1N=C(C(C)(C)C)SC=1C1C=CN=C(N)N=1)NS(C1C(=CC=CC=1F)F)(=O)=O |
NCI Dictionary of Cancer Terms | dabrafenib mesylate |
FDA UNII | B6DC89I63E |
NCI Drug Dictionary | dabrafenib mesylate |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H319-H335-H302+H312+H332-H315 | |||||||||
Precautionary statements | P301+P312-P302+P352-P305+P351+P338 | |||||||||
HS Code | 2935909099 | |||||||||
NFPA 704 |
|
Dabrafenib Mesylate price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Tocris | 7223 | Dabrafenibmesylate ≥98%(HPLC) | 1195768-06-9 | 50 | $149 | 2021-12-16 | Buy |
TRC | D101005 | DabrafenibMesylate | 1195768-06-9 | 25mg | $150 | 2021-12-16 | Buy |
Biosynth Carbosynth | FD158016 | Dabrafenib mesylate | 1195768-06-9 | 25mg | $187.5 | 2021-12-16 | Buy |
ChemScene | CS-1641 | DabrafenibMesylate 99.94% | 1195768-06-9 | 50mg | $100 | 2021-12-16 | Buy |
Apolloscientific | BISN0172 | Dabrafenib Mesylate | 1195768-06-9 | 10mg | $129 | 2021-12-16 | Buy |
Dabrafenib Mesylate Chemical Properties,Uses,Production
Description
Dabrafenib Mesylate(1195768-06-9) is a salt form of Dabrafenib. Dabrafenib is an inhibitor of certain mutated forms of BRAF kinase, several of which may be associated with stimulating tumour growth (e.g. the BRAF V600E mutation), and Dabrafenib is also an inhibitor of BRAF V600-mutation positive cancer cell growth, both in vitro and in vivo.
Description
Dabrafenib mesylate, sold by GlaxoSmithKline under the trade name Tafinlar, was approved by the U.S. FDA in May 2013 for the treatment of metastatic BRAF-mutant melanoma. Dabrafenib reversibly inhibits the BRAF(V600E) mutant kinase as a selective ATP-competitive inhibitor which results in tumor regression.
Uses
Dabrafenib is an inhibitor of mutated BRAF kinase and has clinical activity with a manageable safety profile in clinical trials of phase 1 and 2 in patients with BRAF(V600)-mutated metastatic melanoma.
Definition
ChEBI: A methanesulfonate (mesylate) salt prepared from equimolar amounts of dabrafenib and methanesulfonic acid. Used for treatment of metastatic melanoma.
Synthesis
Commercially available fluoroaniline 40 was first converted to sulfonamide 42 in 91% yield by treatment with 2,5-difluorobenzenesulfonyl chloride (41) in the presence of pyridine. Next, deprotonation of 2-chloro-4-methylpyrimidine (43) with lithium bis(trimethylsilyl)amide (LHMDS) followed by addition to ester 42 afforded chloropyrimidine 44 in 72% yield. Bromination followed by thiazole formation through the use of 2,2-dimethylpropanethioamide gave the penultimate target 45 in 80% over two steps. Chloropyrimidine 45 was subjected to SNAr conditions with ammonium hydroxide to furnish the aminopyrimidine in 88% yield, and this was followed by exposure to methanesulfonic acid to afford dabrafenib mesylate (VI) in 85% yield.
target
Raf
storage
Store at -20°C
References
[1]namba h, nakashima m, hayashi t, hayashida n, maeda s, rogounovitch ti, ohtsuru a, saenko va, kanematsu t, yamashita s. clinical implication of hot spot braf mutation, v599e, in papillary thyroid cancers. j. clin. endocrinol. metab. 2003; 88 (9): 4393–7.
[2]tan yh, liu y, eu kw, ang pw, li wq, salto-tellez m, iacopetta b, soong r. detection of braf v600e mutation by pyrosequencing. pathology 2008; 40 (3): 295–8.
[3]davies h, bignell gr, cox c, et al. mutations of the braf gene in human cancer. nature. 2002; 417: 949-954.
[4]ma xh, piao sf, dey s, mcafee q, karakousis g, villanueva j, hart ls, levi s, hu j, zhang g, lazova r, klump v, pawelek jm, xu x, xu w, schuchter lm, davies ma, herlyn m, winkler j, koumenis c, amaravadi rk. targeting er stress-induced autophagy overcomes braf inhibitor resistance in melanoma. j clin invest. 2014; 124(3): 1406-17.
Dabrafenib Mesylate Preparation Products And Raw materials
Raw materials
1of2
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
AFINE CHEMICALS LIMITED | +86-0571-85134551 | info@afinechem.com | China | 15394 | 58 |
Beijing Mesochem Technology Co.,Ltd | +8613651027935 | rachel@mesochem.com | China | 191 | 58 |
Zison Pharmaceutical (Shandong) Co., Ltd. | +86-0086-531-88259693 +86-18660188356 | tracy.li@zisonpharm.com | China | 57 | 58 |
Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 | Mandy@hangyubiotech.com | China | 10991 | 58 |
Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 20293 | 58 |
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 | sales@sjar-tech.com | China | 251 | 58 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9355 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32836 | 60 |
Anqing Chico Pharmaceutical Co., Ltd. | 15380796838 | chloewu@chicopharm.cn | CHINA | 341 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29888 | 58 |
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View Lastest Price from Dabrafenib Mesylate manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-09-20 | Dabrafenib Mesylate
1195768-06-9
|
US $1.00 / g | 5g | More Than 99% | 100kg/Month | BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | ||
2024-08-27 | Dabrafenib Mesylate(GSK-2118436B)
1195768-06-9
|
US $80.00-800.00 / kg | 10kg | 0.99 | 20tons | Zibo Hangyu Biotechnology Development Co., Ltd | ||
2024-07-17 | Dabrafenib mesylate
1195768-06-9
|
US $0.00-0.00 / kg | 1kg | >99.5% by HPLC | 100kg/month | Zison Pharmaceutical (Shandong) Co., Ltd. |
- Dabrafenib Mesylate
1195768-06-9
- US $1.00 / g
- More Than 99%
- BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
- Dabrafenib Mesylate(GSK-2118436B)
1195768-06-9
- US $80.00-800.00 / kg
- 0.99
- Zibo Hangyu Biotechnology Development Co., Ltd
- Dabrafenib mesylate
1195768-06-9
- US $0.00-0.00 / kg
- >99.5% by HPLC
- Zison Pharmaceutical (Shandong) Co., Ltd.