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Dabrafenib Mesylate

Dabrafenib Mesylate Structure
Dabrafenib Mesylate structure
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
Last updated:2024-04-03 10:16:21
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Dabrafenib Mesylate Properties

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)  GHS hazard pictograms
GHS07
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
0
3 0

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
Product number Packaging Price Buy
7223 50 $149 Buy
D101005 25mg $150 Buy
FD158016 25mg $187.5 Buy
CS-1641 50mg $100 Buy
BISN0172 10mg $129 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.

Synthesis_1195768-06-9

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 synthesis

75-75-2
1195765-45-7
1195768-06-9
Synthesis of Dabrafenib Mesylate from Methanesulfonic acid and Dabrafenib

Dabrafenib Mesylate Preparation Products And Raw materials

Raw materials

2,6-Difluorobenzenesulfonyl chloride N-(3-(2-(2-chloropyriMidin-4-yl)acetyl)-2-fluorophenyl)-2,6-difluorobenzenesulfonaMide Dabrafenib N-{3-[5-(2-chloro-4-pyriMidinyl)-2-(1,1-diethylethyl)-1,3-thiazol-4-yl]-2-fluoraphenyl}-2,6-difluorobenzenesulfonaMide Methyl 3-(2,6-difluorophenylsulfonamido)-2-fluorobenzoate
methyl 3-amino-2-fluorobenzoate Methanesulfonic acid

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Preparation Products

Dabrafenib Mesylate Suppliers

Global( 183)Suppliers
Supplier Tel Email Country ProdList Advantage
AFINE CHEMICALS LIMITED 		0571-85134551 info@afinechem.com CHINA 15377 58
Beijing Mesochem Technology Co.,Ltd
+8613651027935 rachel@mesochem.com China 191 58
Zison Pharmaceutical (Shandong) Co., Ltd.
+86-0086-531-88259693 +86-18660188356 maguanglei@zisonpharm.com China 53 58
Zibo Hangyu Biotechnology Development Co., Ltd 		+86-0533-2185556 +8617865335152 Mandy@hangyubiotech.com China 11013 58
Henan Fengda Chemical Co., Ltd 		+86-371-86557731 +86-13613820652 info@fdachem.com China 7845 58
Hangzhou FandaChem Co.,Ltd. 		008657128800458; +8615858145714 fandachem@gmail.com China 9348 55
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Anqing Chico Pharmaceutical Co., Ltd. 		15380796838 chloewu@chicopharm.cn CHINA 341 58
career henan chemical co 		+86-0371-86658258 sales@coreychem.com China 29914 58
Hubei xin bonus chemical co. LTD 		86-13657291602 linda@hubeijusheng.com CHINA 22968 58
Supplier Advantage
AFINE CHEMICALS LIMITED 		58
Beijing Mesochem Technology Co.,Ltd
58
Zison Pharmaceutical (Shandong) Co., Ltd.
58
Zibo Hangyu Biotechnology Development Co., Ltd 		58
Henan Fengda Chemical Co., Ltd 		58
Hangzhou FandaChem Co.,Ltd. 		55
ATK CHEMICAL COMPANY LIMITED 		60
Anqing Chico Pharmaceutical Co., Ltd. 		58
career henan chemical co 		58
Hubei xin bonus chemical co. LTD 		58

Related articles

View Lastest Price from Dabrafenib Mesylate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Dabrafenib Mesylate pictures 2024-03-26 Dabrafenib Mesylate
1195768-06-9
 US $6.00-0.20 / KG 1KG 98% g-kg-tons, free sample is available Henan Fengda Chemical Co., Ltd
Dabrafenib Mesylate(GSK-2118436B) pictures 2024-01-02 Dabrafenib Mesylate(GSK-2118436B)
1195768-06-9
 US $80.00-800.00 / kg 10kg 0.99 20tons Zibo Hangyu Biotechnology Development Co., Ltd
Dabrafenib mesylate pictures 2023-12-01 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 pictures
  • Dabrafenib mesylate
    1195768-06-9
  • US $0.00-0.00 / kg
  • ＞99.5% by HPLC
  • Zison Pharmaceutical (Shandong) Co., Ltd.

Dabrafenib Mesylate Spectrum

Dabrafenib Mesylate(GSK-2118436B)(1195768-06-9)1HNMR

1195768-06-9(Dabrafenib Mesylate)Related Search:

Methanesulfonic acid Phentolamine mesilate Osimertinib mesylate Selumetinib Cabozantinib
Dabrafenib Trametinib Crizotinib AZD-9291 Vandetanib

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Dabrafenib Mesylate(GSK-2118436B) GSK 2118436 Mesylate GSK 2118436B GSK2118436 Mesylate GSK-2118436 Mesylate Dabrafenib Mesylate (API) GSK 2118436 methanesulfonate salt N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-benzenesulfonamide methanesulfonate N-(3-(5-(2-Aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide methanesulfonate GSK2118436 Ms salt, Dabrafenib Ms salt, GSK2118436A Ms salt Debrafenib Mesylate (API) Dabrafenib, Methanesulfonate Salt Dabrfenib Mesylate N-(3-(5-(2-Aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzen Dabrafenib Mesylate (GSK-2118436) Dapafini mesylate DABRAFENIB MESYLATE (GSK 2118436B);GSK-2118436 MESYLATE;GSK2118436 MESYLATE;GSK 2118436 MESYLATE Benzenesulfonamide, N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-, methanesulfonate (1:1) abrafenibmesylate Dabrafenib Mesylate (GSK2118436 Mesylate N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide methanesulfonic acid Dabrafenib Mesylate Dalafenib methanesulfonate 1195768-06-9 C23H20F3N5O2S2CH4O3S C24H24F3N5O5S3 Raf B protein kinase inhibitor API