ChemicalBook > CAS DataBase List > Tozasertib

Tozasertib

Product Name
Tozasertib
CAS No.
639089-54-6
Chemical Name
Tozasertib
Synonyms
VE465;VX 680;VE 465;CS-176;VE-465;VX-860;MK 0457;Tozasertib;L-001281814;VX-680/MK-0457
CBNumber
CB51513746
Molecular Formula
C23H28N8OS
Formula Weight
464.59
MOL File
639089-54-6.mol
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Tozasertib Property

Melting point:
248-253°C (dec.)
Density 
1.40±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
Soluble in DMSO (up to 100 mg/ml).
form 
powder
pka
14.09±0.70(Predicted)
color 
white to beige
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2158
Product name
VX-680
Purity
≥98% (HPLC)
Packaging
10mg
Price
$76
Updated
2024/03/01
Cayman Chemical
Product number
13600
Product name
MK-0457
Purity
≥98%
Packaging
25mg
Price
$86
Updated
2024/03/01
Cayman Chemical
Product number
13600
Product name
MK-0457
Purity
≥98%
Packaging
50mg
Price
$161
Updated
2024/03/01
Cayman Chemical
Product number
13600
Product name
MK-0457
Purity
≥98%
Packaging
100mg
Price
$302
Updated
2024/03/01
Cayman Chemical
Product number
13600
Product name
MK-0457
Purity
≥98%
Packaging
250mg
Price
$546
Updated
2024/03/01
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Tozasertib Chemical Properties,Usage,Production

Description

The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis. MK-0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. MK-0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s = <10 μM) and blocks the growth of tumors in a rodent model of cancer (80 mg/kg), inhibiting histone H3 phosphorylation and increasing apoptosis. By depleting Aurora activity, MK-0457 disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.

Chemical Properties

White Solid

Uses

Tozasertib is used as a multikinase inhibitor once used for cancer treatment.

Definition

ChEBI: N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide is a N-arylpiperazine.

Biochem/physiol Actions

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.

References

1) Harrington et al. (2004), VX-680, a potent and selective small molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo; Nat. Med., 10 262 2) Fei et al. (2010), Activity of the Aurora kinase inhibitor VX-680 against Bcr/Abl-positive acute lymphoblastic leukemias; Mol. Cancer Ther., 9 1318 3) Dewerth et al. (2012), In vitro evaluation of the Aurora kinase inhibitor VX-680 for Hepatoblastoma; Pediatr. Surg. Int., 28 579

Tozasertib Preparation Products And Raw materials

Raw materials

Preparation Products

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Tozasertib Suppliers

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View Lastest Price from Tozasertib manufacturers

Career Henan Chemical Co
Product
Tozasertib 639089-54-6
Price
US $1.00/g
Min. Order
100g
Purity
99%
Supply Ability
G/KG/T
Release date
2019-12-20

639089-54-6, TozasertibRelated Search:

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  • Cyclopropane carboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino) -pyrimidin-2ylsulphanyl]-phenyl}-amide
  • VX-680/MK-0457
  • N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)-6-(1-methylpiperidin-4-ylamino)pyrimidin-2-ylthio)phenyl)cyclopropanecarboxamide
  • MK 0457
  • N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide
  • Tozasertib
  • VX 680
  • Cyclopropanecarboxamide, N-(4-((4-(4-methyl-1-piperazinyl)-6-((5-methyl-1H-pyrazol-3-yl)amino)-2-pyrimidinyl)thio)phenyl)-
  • VX680;MK0457;VX 680 (MK 0457;TOZASERTIB)
  • CS-176
  • VE 465
  • VE465
  • VE-465
  • VX680; VX 680; VX-680; MK0457; MK 0457; MK-0457; VE465; VE-465; VE 465; TOZASERTIB
  • TOZASERTIB;MK-0457;MK0457;VX680;VX 680;MK 0457
  • N-(4-(4-(5-Methyl-1H-pyrazol-3-ylamino)-6-(1-methylpiperidin-4-ylamino)pyrimidin-2-ylthio)phen
  • N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)-6-(4-methylpiperazin-1-yl)pyrimidin-2-ylthio)phenyl)cyclopropanecarboxamide
  • Tozasertib N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide
  • VX-680(Tozasertib)
  • Tozasertib(MK-0457,VX-680)
  • VX-860
  • N-[4-({4-[(3-METHYL-1H-PYRAZOL-5-YL)AMINO]-6-(4-METHYLPIPERAZIN-1-YL)PYRIMIDIN-2-YL}SULFANYL)PHENYL]CYCLOPROPANECARBOXAMIDE
  • tozasertib (MK-0457)
  • MK-0457,Tozasertib
  • Cyclopropanecarboxylic acid N-(4-((4-(4-methylpiperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)pyrimidin-2-yl)sulfanyl)phenyl)amide
  • L-001281814
  • Tozasertib/VX-680
  • N-(4-(4-(3-methyl-1H-pyrazol-5-ylamino)-6-(4-methylpiperazin-1-yl)pyrimidin-2-ylthio)phenyl)cyclopropanecarboxamide
  • VX-680 (MK-0457)(Tozasertib)
  • Tozasertib￡VX680￡MK0457
  • Tozasertib Free Base
  • N-[4-[[4-(4-Methylpiperazin-1-yl)-6-[(5-Methyl-1H-pyrazol-3-yl)aMino]pyriMidin-2-yl]thio]phenyl]cyclopropanecarboxaMide
  • VX-680 (Tozasertib, MK-0457)
  • Tozasertib USP/EP/BP
  • N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
  • MK-0457 Tozasertib VX-680
  • 639089-54-6
  • C24H30N8OS
  • C23H28N8OS
  • Inhibitors
  • A multikinase inhibitor.
  • Inhibitor
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Mutagenesis Research Chemicals
  • Pharmaceuticals