[CAS NO. 945595-80-2] AMG-900

Name: AMG-900
Brand: Arctom Scientific
SKU: SLK-S2719

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [945595-80-2]

Store

Catalog

SLK-S2719

Brand

Selleck

CAS

945595-80-2

DESCRIPTION [945595-80-2]

Overview

MDL	MFCD18633194
Molecular Weight	503.58
Molecular Formula	C28H21N7OS
SMILES	N(C=1C2=C(C(=NN1)C=3SC=C(C)C3)C=CC=C2)C4=CC=C(OC5=C(C=CC=N5)C6=NC(N)=NC=C6)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9858 mL	9.9289 mL	19.8578 mL
5 mM	0.3972 mL	1.9858 mL	3.9716 mL
10 mM	0.1986 mL	0.9929 mL	1.9858 mL
50 mM	0.0397 mL	0.1986 mL	0.3972 mL

Description

AMG 900 is a potent and highly selective pan- inhibitor for Aurora A/B/C with of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.

Targets

Aurora C ^[1] (Cell-free assay)	Aurora B ^[1] (Cell-free assay)	Aurora A ^[1] (Cell-free assay)	p38α ^[1] (Cell-free assay)
1 nM	4 nM	5 nM	53 nM

In vitro

AMG 900 is a novel class of ATP-competitive phthalazinamine small molecule inhibitors of aurora kinases. In HeLa cells, AMG 900 inhibits autophosphorylation of aurora-A and -B as well as phosphorylation of histone H3 on Ser, a proximal substrate of aurora-B. The predominant cellular response of tumor cells to AMG 900 treatment is aborted cell division without a prolonged mitotic arrest, which ultimately results in cell death. AMG 900 inhibits the proliferation of 26 tumor cell lines, including cell lines resistant and to other aurora kinase inhibitors (AZD1152, MK-0457, and PHA-739358), at low nanomolar concentrations (about 2- 3 nM). Furthermore, AMG 900 is active in an AZD1152-resistant HCT116 variant cell line that harbors an aurora-B mutation (W221L).

References

[1] Payton M, et al, Cancer Res, 2010, 70(23), 9846-9854.
[2] Huang L, et al, Xenobiotica, 2011, 41(5), 400-408.

Synonyms

1-Phthalazinamine, N-[4-[[3-(2-amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-

N-[4-[[3-(2-Amino-4-pyrimidinyl)-2-pyridinyl]oxy]phenyl]-4-(4-methyl-2-thienyl)-1-phthalazinamine

AMG 900