RAF265|Multiple intracellular kinases inhibitor|CAS# 927880-90-8

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Size	Price	Stock
10mM (in 1mL DMSO)	$155.00	In stock
Evaluation Sample	$28.00	In stock
5mg	$120.00	In stock
25mg	$360.00	In stock

Publications citing ApexBio Products

Nature.
2016 Apr 21;532(7599):398-401.

Nature.
2015 Aug 20;524(7565):309-14.

Cell.
2015 Aug 27;162(5):987-1002.

Cell.
2015 Feb 12;160(4):729-44.

Immunity.
2016 Jan 19;44(1):88-102

Nat Cell Biol.
2015 May;17(5):627-38.

Nat Neurosci.
2015 Oct;18(10):1464-73.

Nat Commun.
2016 Feb 1;7:10492.

J Cell Biol.
2016 Apr 11;213(1):109-25.

Cell Host Microbe.
2016 Jul 13;20(1):13-24.

Proc Natl Acad Sci U S A.
2016 Mar 8;113(10):2585-90.

Proc Natl Acad Sci U S A.
2015 Jun 30;112(26):E3365-73.

Proc Natl Acad Sci U S A.
2015 Jul 28;112(30):9412-7.

Autophagy.
2016 Jul 2;12(7):1129-52.

Cancer Res canres.
2946.2015.

Elife.
2016 Jan 14;5. pii: e12203.

Nucleic Acids Res.
2016 Feb 18;44(3):e2.

EMBO Rep.
2015 Sep;16(9):1114-30.

Oncogene.
2016 Mar 21.

Cell Rep.
2015 Sep 29;12(12):1986-96.

Cell Death Differ.
2016 Jun;23(6):1026-37.

Cell Death Differ.
2016 Jan;23(1):76-88.

Diabetes Obes Metab.
2015 Apr;17(4):403-13.

Oncotarget.
2015 Jan 20;6(2):1171-89.

J Neurosci.
2015 Sep 23;35(38):13244-56.

Sci Signal.
2014 Dec 23;7(357):ra122.

Mol Ther.
2015 Sep;23(9):1475-85.

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2016 Feb;57 Suppl 1:75S-80S.

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2015 Apr 1;106(1):153-62.

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2015 Nov;72(22):4399-407.

Anal Chem.
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Quality Control

Quality Control & MSDS

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Purity = 98.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

Related Biological Data

Biological Activity

Description	RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM.
Targets	B-Raf	VEGFR2
IC50	3-60 nM	30 nM (EC50)

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Chemical Properties

Cas No.	927880-90-8	SDF	Download SDF
Synonyms	CHIR-265;RAF 265;RAF-265;CHIR265
Chemical Name	1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine
Canonical SMILES	CN1C2=C(C=C(C=C2)OC3=CC(=NC=C3)C4=NC=C(N4)C(F)(F)F)N=C1NC5=CC=C(C=C5)C(F)(F)F
Formula	C₂₄H₁₆F₆N₆O	M.Wt	518.43
Solubility	Soluble in DMSO > 10 mM	Storage	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

Background

RAF265, also known as CHIR-265, is a novel and orally available small molecule inhibitor of multiple intracellular kinases, including BRAFV600E, BRAF (wild-type), c-RAF, vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF) 1R, RET, c-KIT, SRC and STE20, with half maximal inhibitory concentration IC50 ranging from less than 20 nmo/L to more than 100 nmol/L, in which it exhibits the highest potency for BRAFV600E and VEGFR2 with half maximal effective concentration EC50 of 0.14 μM and 0.19 μM respectively. RAF265 has been found to inhibit proliferation of melanoma and colorectal cancer cell lines with active BRAF mutations and time- and dose-dependently suppress tumor regression in BRAFV600E melanoma and colorectal cancer xenograft models.

References:
[1]Huang T1, Karsy M, Zhuge J, Zhong M, Liu D. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 25;6:30. doi: 10.1186/1756-8722-6-30.
[2]Garcia-Gomez A1, Ocio EM, Pandiella A, San Miguel JF, Garayoa M. RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications. Invest New Drugs. 2013 Feb;31(1):200-5. doi: 10.1007/s10637-012-9845-3. Epub 2012 Jul 7.
[3]Su Y1, Vilgelm AE, Kelley MC, Hawkins OE, Liu Y, Boyd KL, Kantrow S, Splittgerber RC, Short SP, Sobolik T, Zaja-Milatovic S, Dahlman KB, Amiri KI, Jiang A, Lu P, Shyr Y, Stuart DD, Levy S, Sosman JA, Richmond A. RAF265 inhibits the growth of advanced human melanoma tumors. Clin Cancer Res. 2012 Apr 15;18(8):2184-98. doi: 10.1158/1078-0432.CCR-11-1122. Epub 2012 Feb 20.