XL147(SAR245408) Inhibitor CAS No. 956958-53-5

Cat. No.	Name	Size	Price
KI3070	XL147(SAR245408)	5 mg	$312
	XL147(SAR245408)	10 mg	$390
	XL147(SAR245408)	20 mg	$676
	XL147(SAR245408)	50 mg	$1040
	XL147(SAR245408)	100 mg	$1820
	XL147(SAR245408)	200 mg	$3120
	XL147(SAR245408)	1 g	$10400

Chemical Characteristic

Product Name	XL147(SAR245408)
CAS No.	956958-53-5
Molecular Weight	448.52
Formula	C₂₁H₁₆N₆O₂S₂
Chemical Name	N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide
Smiles	c1(ccc(cc1)C)S(=O)(=O)Nc1nc2c(nc1Nc1cc3nsnc3cc1)cccc2
Chemical Structure

Biological activities

XL147 (SAR245408) is a PI3K inhibitor.^[1] The IC50s of XL147 are 39, 383, 36 and 23 nM against PI3Kα, ??3?β, PI3Kδ and ??3Kγ, respectively.^[1][2] XL147 inhibits the phosphorylation of downstream effectors Akt and S6 ribosomal protein (S6RP) and targets only PI3 isoforms (PI3Kα , ??3?β , PI3? and ??3γ). XL147 has been widely used as antitumor agents for the treatment of solid tumors, lymphoma and endometrial or hormone receptor-positive breast cancer.^[3] In vitro, in the HER2-overexpressing human breast cancer cell lines, XL147 abrogates AKT and S6 phosphorylation, and also induces the expression and phosphorylation of HER3 and other RTKs.^[4]In vivo, in the athymic mice bearing BT474 xenografts, the antitumor effect of XL147 against HER2-dependent xenografts can be enhanced by addition of trastuzumab or lapatinib.^[4]

Protocols

In vivo: XL147 (SAR245408) is dissolved in DMSO.^[4]

References

[1]Baselga J. Targeting the phosphoinositide-3 (PI3) kinase pathway in breast cancer. Oncologist. 2011;16 Suppl 1:12-19. [2]Chakrabarty A, et al. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc Natl Acad Sci U S A. 2012 ;109(8):2718-2723. [3]Debussche, Laurent, et al. Compositions comprising a pi3k inhibitor and a mek inhibitor and their use for treating cancer. WIPO Patent Application PCT/US2011/063871. [4]Chakrabarty A, et al. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc Natl Acad Sci U S A. 2012;109(8):2718-2723.

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