SB590885 405554-55-4

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Molecular Weight:

453.54 SB590885 is a Potent B-Raf Inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.


Biological Activity


SB590885 displays significant selectivity for B-Raf over c-Raf with Ki of 0.16 nM over 1.72 nM. SB-590885 is a more Potent Inhibitor than the
previously described Raf/VEGFR kinase inhibitor BAY 439006 (Ki = 38 nM for mutant B-Raf, 6 nM for c-Raf). SB590885 displays potent
selectivity over 46 Other kinases. Unlike the multi-kinase inhibitor
BAY43-9006, SB590885 stabilizes the oncogenic B-Raf kinase domain in an
active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M
cells expressing oncogenic B-RafV600E, SB590885 treatment potently
inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM,
and 190 nM, respectively, and consistently, inhibits the proliferation
with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM,
respectively.


SB590885 decreases anchorage-independent growth of
melanoma cell lines in a BRAF mutant-selective manner. SB590885
displays high affinity for B-Raf with Kd of 0.3 nM. Most of the
melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4
mutations (451Lu, WM35, and WM983) are highly sensitive to SB590885 with
IC50 of


Administration of SB590885 potently decreases tumorigenesis in murine
xenografts established from mutant B-Raf-expressing A375P melanoma
cells, and modestly inhibits tumor growth.


Protocol(Only for Reference)


Cell Assay: [1]

Cell lines	Colo205, HT29, A375P, SKMEL28, and MALME-3M
Concentrations	Dissolved in DMSO, final concentrations ~10 μM
Incubation Time	72 hours
Method	Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for Cell Cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.

Animal Study: [1]

Animal Models	Female nude mice injected s.c. with of A375P cells
Formulation	Dissolved in vehicle [2% N,N-dimethylacetamide, 2% Cremophor EL, and 96% acidified water (pH f4-5)]
Dosages	50 mg/kg/day
Administration	Injection i.p.
Solubility	2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0, 30 mg/mL
* 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	453.54
Formula	C27H27N5O2
CAS No.	405554-55-4

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	5 mg/mL (11.02 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0	30 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.

Chemical Name	(E)-5-(2-(4-(2-(dimethylamino)ethoxy)phenyl)-4-(pyridin-4-yl)-1H-imidazol-5-yl)-2,3-dihydroinden-1-one oxime

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Product Categories : MAPK > Raf Inhibitor