639089-54-6 Tozasertib AKSci W9901
 
 
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  W9901    AKSci Reference Standard
Tozasertib, 98% (HPLC)
 
VX-680
MK-0457
IDENTITY
CAS Number:639089-54-6
MDL Number:MFCD13185152
MF:C23H28N8OS
MW:464.59
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:168-174°C
Density:1.406
Refractive Index:1.708
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO 93 mg/mL
Application(s):pan-Aurora inhibitor
Form:Free base

REVIEW
 Tozasertib (MK 0457; VX 680) is a synthetic, small-molecule pan-Aurora kinase inhibitor, mostly against Aurora A and less potent towards Aurora B/Aurora C with potential antitumor activity. It binds to and inhibits Aurora kinases, thereby inducing apoptosis in tumor cells in which AKs are overexpressed.

REFERENCES
[1]Harrington EA, Bebbington D, Moore J, Rasmussen RK, Ajose-Adeogun AO, Nakayama T, Graham JA, Demur C, Hercend T, Diu-Hercend A, Su M, Golec JM, Miller KM. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. (2004) Mar;10(3): 262-7.
[2] Gizatullin Farid; Yao Yao; Kung Victor; Harding Matthew W; Loda Massimo; Shapiro Geoffrey I. The Aurora kinase inhibitor VX-680 induces endoreduplication and apoptosis preferentially in cells with compromised p53-dependent postmitotic checkpoint function. Cancer Research. (2006) 66(15): 7668-77.
[3] Li Y, Zhang ZF, Chen J, Huang D, Ding Y, Tan MH, Qian CN, Resau JH, Kim H, Teh BT. VX680/MK-0457, a potent and selective Aurora kinase inhibitor, targets both tumor and endothelial cells in clear cell renal cell carcinoma. Am J Transl Res. (2010) May 20;2(3): 296-308.
[4] Charrier, Jean-Damien; Mazzei, Francesca; Kay, David; Miller, Andrew Processes for preparing 6-pyrazolylpyrimidines as inhibitors of protein kinase, in particular Aurora kinases, by nucleophilic substitution PCT Int. Appl. (2003), WO 2004000833 A1 20031231.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501

Current as of May 13, 2024

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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