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Merck
Összes fotó(1)

Fontos dokumentumok

Összes dokumentáció megtekintése

SML2158

Sigma-Aldrich

VX-680

≥98% (HPLC)

Szinonimák:

MK 0457, MK-0457, MK0457, N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide, Tozasertib, VX 680, VX680

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez
Összes fotó(1)

About This Item

Tapasztalati képlet (Hill-képlet):
C23H28N8OS
CAS-szám:
639089-54-6
Molekulatömeg:
464.59
MDL-szám:
MFCD13185152
UNSPSC kód:
12352200
NACRES:
NA.77

Teszt

≥98% (HPLC)

Forma

powder

szín

white to beige

oldhatóság

DMSO: 2 mg/mL, clear

tárolási hőmérséklet

2-8°C

SMILES string

O=C(C1CC1)NC(C=C2)=CC=C2SC3=NC(N4CCN(C)CC4)=CC(NC5=NNC(C)=C5)=N3

InChI

1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29)

Nemzetközi kémiai azonosító kulcs

GCIKSSRWRFVXBI-UHFFFAOYSA-N

Biokémiai/fiziológiai hatások

ATP site-targeting potent aurora kinase and Abl inhibitor with in vitro and in vivo anticancer efficacy.
VX-680 is an ATP site-targeting potent aurora kinase inhibitor (Aurara A/B/C Ki(app) = 0.6/18/4.6 nM) that affects FLT3, BCR-Abl, BCR-Abl (T315I), Lck, ITK, Src, and Fyn only at higher concentrations (Ki(app) = 30, 30, 42, 80, 220, 350, 520 nM, respectively) and exhibits little inhibitory potency toward 52 other kinases (Ki(app) >1 μM). VX-680 exhibits potent antiproliferation activity in a wide variety of cancer cultures (IC50 from 15 to 113 nM) as a result of cell cycle arrest and apoptosis induction, as well as causes tumor retardation (by 98% on day 13; 75 mg/kg b.i.d i.p.; HL-60 in mice) and regression (2 mg/kg/h 3 d/wk i.v. infusion; HCT116 in rats) in vivo. Crystallography data reveal a tight association of VX-680 with a hydrophobic pocket present only in a closed, inactive kinase conformation, which forms the basis of its selectivity profile, including its activity toward wild-type and the Imatinib-resistant (T315I) Abl.

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

Válasszon a legfrissebb verziók közül:

Analitikai tanúsítványok (COA)

Lot/Batch Number
0000225170
0000225170
0000281616
0000281616
0000159342

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Dokumentumtár megtekintése

Farid Gizatullin et al.
Cancer research, 66(15), 7668-7677 (2006-08-04)
VX-680 is a potent inhibitor of Aurora kinases that induces the accumulation of cells with > or =4N DNA content, followed by cell death. Here, we define the role of p53 and p21(Waf1/Cip1) in cell cycle perturbations following exposure to
Inger Brandsma et al.
Toxicological sciences : an official journal of the Society of Toxicology, 177(1), 202-213 (2020-07-04)
Understanding the mode-of-action (MOA) of genotoxic compounds and differentiating between direct DNA interaction and indirect genotoxicity is crucial for their reliable safety assessment. ToxTracker is a stem cell-based reporter assay that detects activation of various cellular responses that are associated
G M T Cheetham et al.
Cancer letters, 251(2), 323-329 (2007-01-24)
The small molecule inhibitor of the Aurora-family of protein kinases VX-680 or MK-0457, demonstrates potent anti-cancer activity in multiple in vivo models and has recently entered phase II clinical trials. Although VX-680 shows a high degree of enzyme selectivity against
Mindy I Davis et al.
Nature biotechnology, 29(11), 1046-1051 (2011-11-01)
We tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are
Sukumar Sarkar et al.
Molecular cancer research : MCR, 15(8), 1063-1072 (2017-05-26)
Reducing the levels of the androgen receptor (AR) is one of the most viable approaches to combat castration-resistant prostate cancer. Previously, we observed that proteasomal-dependent degradation of AR in response to 2-methoxyestradiol (2-ME) depends primarily on the E3 ligase C-terminus
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