Dabrafenib (GSK2118436)

貨號 Cat. No.: S2807
規格 Size: 5~200mg
品牌 Brand: Selleckchem

Description

Catalog No.S2807

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. Phase 3.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 226	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 113	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 163	In stock	0 1 2 3 4 5 6 7 8 9 10
20mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 504	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

Description	Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. Phase 3.
Targets	B-raf	B-Raf^V600E	c-Raf
IC50	3.2 nM	0.8 nM	5.0 nM ^[1]
In vitro	Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-Raf^V600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-Raf^V600E. ^[1]
In vivo	Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. ^[1]
Features

Protocol(Only for Reference)

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01682083	Recruiting	Melanoma	GlaxoSmithKline	2013-01	Phase 3
NCT01738451	Recruiting	Cancer	GlaxoSmithKline	2013-01	Phase 1
NCT01677741	Recruiting	Neoplasms, Brain	GlaxoSmithKline	2013-02	Phase 1
NCT01767454	Recruiting	Solid Tumours	GlaxoSmithKline	2013-02	Phase 1
NCT01721603	Recruiting	BRAFV600E Melanoma Patients	University of California, San Francisco\|GlaxoSmithKline	2013-04	Phase 2

Chemical Information

Download Dabrafenib (GSK2118436) SDF

Molecular Weight (MW)	519.56
Formula	C₂₃H₂₀F₃N₅O₂S₂
CAS No.	1195765-45-7

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	30 mg/mL (57 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	8 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.