VX-680 Inhibitor CAS No. 639089-54-6

Cat. No.	Name	Size	Price
KI0251	VX-680	25 mg	$234
	VX-680	100 mg	$592
	VX-680	250 mg	$752

Chemical Characteristic

Product Name	VX-680
Synonyms	MK-0457, Tozasertib
CAS No.	639089-54-6
Molecular Weight	464.59
Formula	C₂₃H₂₈N₈OS
Chemical Name	N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)-6-(4-methylpiperazin-1-yl)pyrimidin-2-ylthio)phenyl)cyclopropanecarboxamide
Smiles	C1(CC1)C(=O)Nc1ccc(cc1)Sc1nc(cc(n1)Nc1[nH]nc(c1)C)N1CCN(CC1)C
Chemical Structure

Biological activities

VX-680 is a highly potent and selective small-molecule inhibitor of Aurora kinases. ^[1] VX-680 inhibits Aurora A, B and C in an almost identical fashion, and the calculated IC50 values are 36, 18 and 25 nM, respectively. ^[2] VX-680 also inhibits three Aurora kinases, with apparent inhibition constant (K_{i(app)) values of 0.6, 18 and 4.6 nM for Aurora-A, Aurora-B and Aurora-C, respectively. VX-680 shows greater than 100-fold selectivity for the Aurora-A kinase over 55 other kinases tested, the only exception being Fms-related tyrosine kinase-3 (FLT-3; K_{i(app) = 30 nM). In vitro, VX-680 suppresses histone H3 phosphorylation on Ser10 in human cells, indicating that Aurora kinases are inhibited. VX-680 causes accumulation of cells with 4N DNA content and potently inhibits the proliferation of a wide variety of tumor cell types (HCT116, LS174T, HL60, MDA-MB-231, ZR-75-1, MCF-7, PC3, MIA PaCa2, A375, HeLa) with IC50 values ranging from 15 to 113 nM. VX-680 completely ablates colony formation of primary leukemic cells from patients with AML (CFU-L) who are refractory to standard therapies. VX-680 is extremely potent in CFU-L, with IC50 values in the range of 35-100 nM. VX-680 also abolishes colony formation of primary leukemic cells possessing internal tandem duplication (ITD) mutations of FLT3. VX-680 inhibits the proliferation of phytohemagglutinin-stimulated primary human lymphocytes with an IC50 of 79 nM. In vivo, VX-680 induces profound inhibition of tumor growth, resulting in regression at well-tolerated doses. VX-680 causes a marked reduction in tumor size in a human AML (HL-60) xenograft model. VX-680 also induces tumor regression in pancreatic and colon xenograft models. In an established human pancreatic (MIA PaCa-2) xenograft model, VX-680 at 50 mg/kg b.i.d i.p. induces regression in seven of ten tumors, with a 22% decrease in mean tumor volume relative to initial tumor size before treatment. VX-680 also exhibits potent antitumor activity when infuses i.v. in nude rats bearing established HCT116 (colon) tumors. ^[1]}}

Protocols

VX-680 is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. ^[1]

References

[1] Harrington EA, et al. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004, 10(3): 262-267. [2] Tyler RK, et al. VX-680 inhibits Aurora A and Aurora B kinase activity in human cells. Cell Cycle. 2007, 6(22): 2846-2854.

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