Cayman MK-0457

Name: Cayman MK-0457
SKU: CAYM-13600-100
Price: 156.00 USD

List Price $156.00 Your Price $156.00

Cayman MK-0457 - CAYM (Additional S&H Or Hazmat Fees May Apply)

NETA PART: CAYM-13600-100

MFG.PART: 13600-100

UNSPSC: 12352200

Manufacturer: Cayman

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Description

Product 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.

WARNING This product is not for human or veterinary use.

Technical Information

Formal Name

N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]-cyclopropanecarboxamide

CAS Number

639089-54-6

Synonyms

Tozasertib
VX-680

Molecular Formula

C₂₃H₂₈N₈OS

Formula Weight

464.6

Purity

≥98%

Formulation

A crystalline solid

Solubility

DMF: 20 mg/mL
DMF:PBS (pH 7) (1:10): 0.1 mg/mL
DMSO: 15 mg/mL

λ_max

253 nm

SMILES

CN1CCN(C2=CC(NC3=NNC(C)=C3)=NC(SC4=CC=C(NC(C5CC5)=O)C=C4)=N2)CC1

InChi Code

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)

InChi Key

GCIKSSRWRFVXBI-UHFFFAOYSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room Temperature in continental US; may vary elsewhere

Stability

≥ 4 years

Specifications

More Information
SKU	CAYM-13600-100
Supplier Part Number	13600-100
UM	EA
UNSPSC	12352200
Manufacturer	Cayman
MSDS URL	Click here
Temperature	-20
Refrigerated-Frozen	Y
CountryOfOrigin	China
ProductLine	CAYM
Qty	1
MinOrderQty	1
Weight	7.000000
Lead Time	5
Hazardous	N
CAS Number	639089-54-6
Energy Star	No
Green	No
Controlled	N

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NETA PART NO.	Quantity

Cayman MK-0457

Product Description

Technical Information

Shipping & Storage Information

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