Dabrafenib Mesylate
Description- Product Name
- 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;Dabrafenib Mesylate (API);Debrafenib Mesylate (API)
- CBNumber
- CB72630077
- Molecular Formula
- C24H24F3N5O5S3
- Formula Weight
- 615.66
- MOL File
- 1195768-06-9.mol
Dabrafenib Mesylate Property
- 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
- InChI
- InChI=1S/C23H20F3N5O2S2.CH4O3S/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25;1-5(2,3)4/h4-11,31H,1-3H3,(H2,27,28,29);1H3,(H,2,3,4)
- 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
Safety
- HS Code
- 2935909099
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 7223
- Product name
- Dabrafenibmesylate
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $149
- Updated
- 2021/12/16
- Product number
- D101005
- Product name
- DabrafenibMesylate
- Packaging
- 25mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- FD158016
- Product name
- Dabrafenib mesylate
- Packaging
- 25mg
- Price
- $187.5
- Updated
- 2021/12/16
- Product number
- CS-1641
- Product name
- DabrafenibMesylate
- Purity
- 99.94%
- Packaging
- 50mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- BISN0172
- Product name
- Dabrafenib Mesylate
- Packaging
- 10mg
- Price
- $129
- Updated
- 2021/12/16
Dabrafenib Mesylate Chemical Properties,Usage,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
Preparation Products
Dabrafenib Mesylate Suppliers
- Tel
- 44-20819178-90 02081917890
- Fax
- (0)2080432064
- info@novachemistry.com
- Country
- United Kingdom
- ProdList
- 4381
- Advantage
- 58
View Lastest Price from Dabrafenib Mesylate manufacturers
- Product
- Dabrafenib Mesylate 1195768-06-9
- Price
- US $1.00/g
- Min. Order
- 5g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-08-09
- Product
- Dabrafenib mesylate 1195768-06-9
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- ＞99.5% by HPLC
- Supply Ability
- 100kg/month
- Release date
- 2023-02-18
- Product
- Dabrafenib Mesylate 1195768-06-9
- Price
- US $0.00/g
- Min. Order
- 10g
- Purity
- 99.9
- Supply Ability
- 20kgs
- Release date
- 2024-05-24