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SB-590885

Catalog No. T2295 CAS 405554-55-4

SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to other human kinases.

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SB-590885, CAS 405554-55-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 268.00
50 mg	In stock	$ 513.00
100 mg	In stock	$ 747.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Purity: 99.06%

Purity: 98.48%

Purity: 95.43%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to other human kinases.
Targets&IC50	B-Raf:0.16 nM(Ki)
In vitro	In mice with A375P melanoma xenografts that express the B-Raf(V600E) variant, SB590885 significantly reduces tumor incidence and exhibits a certain inhibitory effect on tumor growth.
In vivo	SB590885 effectively inhibits ERK phosphorylation (EC50: 28/58/290/58/190 nM) and proliferation (EC50: 0.1/0.87/0.37/0.12/0.15 μM) in Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing the carcinogenic B-RafV600E. Compared to c-Raf (Ki: 1.72 nM), SB590885 displays significantly higher selectivity for B-Raf (Ki: 0.16 nM). Unlike the multikinase inhibitor BAY43-9006, SB590885 stabilizes the active conformation of the oncogenic B-Raf kinase domain and shows a high affinity for B-Raf (Kd: 0.3 nM). Melanoma cell lines with the BRAF V600E mutation but without the CDK4 mutation (451Lu, WM983, and WM35) are highly sensitive to SB590885 (IC50 <1 μM).
Cell Research	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.(Only for Reference)

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.5 mg/mL (27.56 mM)

References and Literature

1. King AJ, et al. Cancer Res, 2006, 66(23), 11100-11105. 2. Takle AK, et al. Bioorg Med Chem Lett, 2006, 16(2), 378-381. 3. Smalley KS, et al. Mol Cancer Ther, 2008, 7(9), 2876-2883.

Citations

1. Xiao Y, Gong Q, Wang W, et al. The combination of Biochanin A and SB590885 potentiates the inhibition of tumour progression in hepatocellular carcinoma. Cancer Cell International. 2020, 20(1): 1-11

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Kinase Inhibitor Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library HIF-1 Signaling Pathway Compound Library Reprogramming Compound Library Target-Focused Phenotypic Screening Library Anti-Colorectal Cancer Compound Library

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Keywords

SB-590885 405554-55-4 MAPK Raf Raf kinases inhibit Inhibitor SB 590885 SB590885 inhibitor

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