Dabrafenib


Catalog No. size PriceQuantity
M6667-2 2mg solid $83
M6667-10 10mg solid $328

Description

Cas:1195765-45-7 (free base)

Product Information

Dabrafenib, also known as GSK2118436 , is an orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity. Dabrafenib selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. B-raf belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. On May 29, 2013, FDA approved this drug.

 

Chemical Formula: C23H20F3N5O2S2

 

Exact Mass: 519.10105

 

Molecular Weight: 519.56 

 

Elemental Analysis: C, 53.17; H, 3.88; F, 10.97; N, 13.48; O, 6.16; S, 12.34

 

Synonym: 

 

GSK2118436A ( Dabrafenib )

GSK 2118436A

GSK-2118436A

GSK2118436B ( Dabrafenib Mesylate )

GSK-2118436B

GSK 2118436B

Trade name: Tafinlar

 

Chemical Name:

N-(3-(5-(2-aminopyrimidin-4-yl)-2-(tert-butyl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide

 

InChi Key:

BFSMGDJOXZAERB-UHFFFAOYSA-N

 

InChi Code:  InChI=1S/C23H20F3N5O2S2/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/h4-11,31H,1-3H3,(H2,27,28,29)

 

Smiles Code:

O=S(C1=C(F)C=CC=C1F)(NC2=CC=CC(C3=C(C4=NC(N)=NC=C4)SC(C(C)(C)C)=N3)=C2F)=O

 

 

Technical Data:

 

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life:>2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells.

 

In Vivo

Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas.

 

 

References

 

  1. Banzi M, De Blasio S, Lallas A, Longo C, Moscarella E, Alfano R, Argenziano G. Dabrafenib: a new opportunity for the treatment of BRAF V600-positive melanoma. Onco Targets Ther. 2016 May 6;9:2725-33. doi: 10.2147/OTT.S75104. eCollection 2016. Review. PubMed PMID: 27226731; PubMed Central PMCID: PMC4866744.

 

  1. Spain L, Julve M, Larkin J. Combination dabrafenib and trametinib in the management of advanced melanoma with BRAFV600 mutations. Expert Opin Pharmacother. 2016;17(7):1031-8. doi: 10.1517/14656566.2016.1168805. Epub 2016 Apr 12. Review. PubMed PMID: 27027150.

 

  1. Zia Y, Chen L, Daud A. Future of combination therapy with dabrafenib and trametinib in metastatic melanoma. Expert Opin Pharmacother. 2015;16(14):2257-63. doi: 10.1517/14656566.2015.1085509. Epub 2015 Sep 2. Review. PubMed PMID: 26331795.

 

  1. Giurcaneanu C, Nitipir C, Popa LG, Forsea AM, Popescu I, Bumbacea RS. Evolution of melanocytic nevi under vemurafenib, followed by combination therapy with dabrafenib and trametinib for metastatic melanoma. Acta Dermatovenerol Croat. 2015;23(2):114-21. Review. PubMed PMID: 26228819.

 

  1. Khoja L, Hogg D. Dabrafenib in the treatment of metastatic or unresectable melanoma. Expert Rev Anticancer Ther. 2015 Mar;15(3):265-76. doi: 10.1586/14737140.2015.1014343. Review. PubMed PMID: 25711514.

 

Products are for research use only. Not for human use.

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