ENMD-2076 L-(+)-Tartaric acid Inhibitor CAS No. 1291074-87-7 - ENMD-2076 L-(+)-Tartaric acid Supplier

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Enmd-2076-l-tartaric-acid

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Cat. No.	Name	Size	Price
KI0990	ENMD-2076 L-(+)-Tartaric acid	5 mg	$272
	ENMD-2076 L-(+)-Tartaric acid	10 mg	$512
	ENMD-2076 L-(+)-Tartaric acid	50 mg	$1552
	ENMD-2076 L-(+)-Tartaric acid	200 mg	$3952

Chemical Characteristic

Product Name	ENMD-2076 L-(+)-Tartaric acid
CAS No.	1291074-87-7
Molecular Weight	525.56
Formula	C₂₅H₃₁N₇O₆
Chemical Name	(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine,L-(+)-Tartaric acid
Smiles	c1(nc(cc(n1)N1CCN(CC1)C)Nc1n[nH]c(c1)C)/C=C/c1ccccc1 C(=O)(C(O)C(O)C(=O)O)O
Chemical Structure

Biological activities

ENMD-2076 is a potent inhibitor of Aurora A and Aurora B with IC50s of 14 and 350 nM, respectively. ENMD-2076 also inhibits Flt3, Flt4 and VEGFR2 with IC50 values of 1.86, 15.9 and 58.2 nM, respectively. In vitro, ENMD-2076 inhibits the growth of a wide range of human solid tumor (including PANC-1, HCT116, A549, HT-29 and MCF7) and hematopoietic cancer cell lines (including MV4:11, U937, Kasumi, MO7e and HL-60) with IC50 values ranging from 0.025 to 0.7 mM. In vivo, ENMD-2076 induces regression or complete inhibition of tumor growth at well-tolerated doses in tumor xenograft models derived from breast, colon, melanoma, leukemia, and multiple myeloma cell lines. ENMD-2076 (75 or 302 mg/kg) prevents the formation of new blood vessels and regress formed vessels in vivo at doses equivalent to those that give substantial activity in MDA-MB-231 tumor xenograft models.^[1] Furthermore, in non-obese diabetic/severe combined immunodeficient mice implanted with H929 human plasmacytoma xenografts, oral treatment with ENMD-2076 (50, 100, 200 mg/kg per day) results in a dose-dependent inhibition of tumour growth.^[2]

References

[1] Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011, 10(1): 126-137. [2] Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010, 150(3): 313-325.

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