Dabrafenib Mesylate

ChemicalBook > CAS DataBase List > 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

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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

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Safety

HS Code: 2935909099

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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.

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N-Bromosuccinimide Price

Tocris

Product number: 7223
Product name: Dabrafenibmesylate
Purity: ≥98%(HPLC)
Packaging: 50
Price: $149
Updated: 2021/12/16

TRC

Product number: D101005
Product name: DabrafenibMesylate
Packaging: 25mg
Price: $150
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FD158016
Product name: Dabrafenib mesylate
Packaging: 25mg
Price: $187.5
Updated: 2021/12/16

ChemScene

Product number: CS-1641
Product name: DabrafenibMesylate
Purity: 99.94%
Packaging: 50mg
Price: $100
Updated: 2021/12/16

Apolloscientific

Product number: BISN0172
Product name: Dabrafenib Mesylate
Packaging: 10mg
Price: $129
Updated: 2021/12/16

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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

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View Lastest Price from Dabrafenib Mesylate manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.

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

Zison Pharmaceutical (Shandong) Co., Ltd.

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

Zison Pharmaceutical (Shandong) Co., Ltd.

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

1195768-06-9, Dabrafenib MesylateRelated Search:

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

Dabrafenib Mesylate (GSK-2118436)

Dabrafenib Mesylate(GSK-2118436B)

Dabrafenib Mesylate

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

Dapafini mesylate

DABRAFENIB MESYLATE (GSK 2118436B);GSK-2118436 MESYLATE;GSK2118436 MESYLATE;GSK 2118436 MESYLATE

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

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

Dalafenib methanesulfonate

1195768-06-9

C23H20F3N5O2S2CH4O3S

C24H24F3N5O5S3

Raf B protein kinase inhibitor

API