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Tozasertib

Tozasertib Structure
Tozasertib structure
CAS No.
639089-54-6
Chemical Name:
Tozasertib
Synonyms
VE465;VX 680;VX-860;CS-176;VE 465;VE-465;MK 0457;Tozasertib;L-001281814;VX-680/MK-0457
CBNumber:
CB51513746
Molecular Formula:
C23H28N8OS
Molecular Weight:
464.59
MDL Number:
MFCD13185152
MOL File:
639089-54-6.mol
Last updated:2023-05-18 11:31:13
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Tozasertib Properties

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).
pka 14.09±0.70(Predicted)
form powder
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.
FDA UNII 234335M86K

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P280-P305+P351+P338

Tozasertib price More Price(36)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML2158 VX-680 ≥98% (HPLC) 639089-54-6 10mg $76 2024-03-01 Buy
Cayman Chemical 13600 MK-0457 ≥98% 639089-54-6 25mg $86 2024-03-01 Buy
Cayman Chemical 13600 MK-0457 ≥98% 639089-54-6 50mg $161 2024-03-01 Buy
Cayman Chemical 13600 MK-0457 ≥98% 639089-54-6 100mg $302 2024-03-01 Buy
Cayman Chemical 13600 MK-0457 ≥98% 639089-54-6 250mg $546 2024-03-01 Buy
Product number Packaging Price Buy
SML2158 10mg $76 Buy
13600 25mg $86 Buy
13600 50mg $161 Buy
13600 100mg $302 Buy
13600 250mg $546 Buy

Tozasertib Chemical Properties,Uses,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

Tozasertib Suppliers

Global( 196)Suppliers
Supplier Tel Email Country ProdList Advantage
Capot Chemical Co.,Ltd. 		571-85586718 +8613336195806 sales@capotchem.com China 29797 60
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Hubei xin bonus chemical co. LTD 		86-13657291602 linda@hubeijusheng.com CHINA 22968 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 47465 58
career henan chemical co 		+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
SIMAGCHEM CORP 		+86-13806087780 sale@simagchem.com China 17367 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
ANHUI WITOP BIOTECH CO., LTD 		+8615255079626 eric@witopchemical.com China 23556 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 29321 58
Supplier Advantage
Capot Chemical Co.,Ltd. 		60
ATK CHEMICAL COMPANY LIMITED 		60
Hubei xin bonus chemical co. LTD 		58
BOC Sciences 		58
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
SIMAGCHEM CORP 		58
TargetMol Chemicals Inc. 		58
ANHUI WITOP BIOTECH CO., LTD 		58
Dideu Industries Group Limited 		58

View Lastest Price from Tozasertib manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Tozasertib pictures 2019-12-23 Tozasertib
639089-54-6
 US $1.00 / g 100g 99% G/KG/T Career Henan Chemical Co
  • Tozasertib pictures
  • Tozasertib
    639089-54-6
  • US $1.00 / g
  • 99%
  • Career Henan Chemical Co

Tozasertib Spectrum

Tozasertib(639089-54-6)1HNMR

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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)- 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 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) 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-[(3-METHYL-1H-PYRAZOL-5-YL)AMINO]-6-(4-METHYLPIPERAZIN-1-YL)PYRIMIDIN-2-YL}SULFANYL)PHENYL]CYCLOPROPANECARBOXAMIDE tozasertib (MK-0457) MK-0457,Tozasertib 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