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 (K_i = 0.6 nM) over Aurora B (K_i = 18 nM) or Aurora C (K_i = 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

Canada 1 China 160 Germany 1 India 2 The Netherlands 1 United Kingdom 4 United States 28 Global 197

Shanghai Boyle Chemical Co., Ltd.

Tel
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Email: sales@boylechem.com
Country: China
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J & K SCIENTIFIC LTD.

Tel: 010-82848833 400-666-7788
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
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Yangzhou Siyu Chemical Co.,Ltd.

Tel: 0514-87325867
Fax: 0086-514-87325867
Email: sales@siyuchem.com
Country: China
ProdList: 370
Advantage: 55

Chembest Research Laboratories Limited

Tel: +86-21-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
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JinYan Chemicals(ShangHai) Co.,Ltd.

Tel: 13817811078
Fax: 86-021-50426522,50426273
Email: sales@jingyan-chemical.com
Country: China
ProdList: 9976
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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.

Tel: 17702719238 17702719238
Email: sales@sun-shinechem.com
Country: China
ProdList: 976
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VDM Biochemicals

Tel: 0330-2528181
Fax: 0330-2528171
Email: sales@vdmbio.com
Country: United States
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Shanghai Paulshine Chemical Co., Ltd.

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Fax: +86-021-37788663
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Shanghai Longsheng chemical Co.,Ltd.

Tel: 021-58099652-8005 13585536065
Fax: 021-58099609
Email: bin.wu@shlschem.com
Country: China
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Chemsky（shanghai）International Co.,Ltd.

Tel: 021-50135380
Email: shchemsky@sina.com
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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:

Tegaserod Levodropropizine Kresoxim-methyl Piperazine METSULFURON METHYL Methyl acrylate Methyl cellulose Methanol N-Aminoethylpiperazine Bensulfuron methyl Piperacillin 2-Ethylhexyl ferulate Methylparaben Pyrazole Trametinib Elexacaftor Methyl VX 702

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