AMG 900

SKU: orb1300819

Description

AMG 900 is a potent, selective pan-Aurora kinase inhibitor with IC50 values of 5, 4, and 1 nM for Aurora A, B, and C, respectively. It demonstrates over 10-fold selectivity against several other kinases. This compound has been utilized in preclinical research to investigate mitotic progression and has shown antitumor activity in various in vivo cancer models.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction

Images & Validation

−

Key Properties

−

CAS Number	945595-80-2
MW	503.58
Purity	98.90%
Formula	C₂₈H₂₁N₇OS
SMILES	Cc1csc(c1)-c1nnc(Nc2ccc(Oc3ncccc3-c3ccnc(N)n3)cc2)c2ccccc12
Target	Tyrosine Kinases,p38 MAPK,Aurora Kinase
Solubility	DMSO:115 mg/mL (228.36 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.93 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);2% DMSO+40% PEG300+5% Tween 80+53% Saline:2 mg/mL (3.97 mM)

Bioactivity

−

Target IC50	Aurora B:4 nM\|Aurora A:5 nM\|Aurora C:1 nM
In Vivo	Oral administration of AMG 900 blocks the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibited the growth of HCT116 tumor xenografts. AMG 900 is broadly active in multiple xenograft models, including 3 multidrugresistant xenograft models, representing 5 tumor types. AMG 900 exhibits a low-to-moderate clearance and a small volume of distribution. Its terminal elimination half-life ranged from 0.6 to 2.4 hours. AMG 900 is well-absorbed in fasted animals with an oral bioavailability of 31% to 107%. Food intake has an effect on rate (rats) or extent (dogs) of AMG 900 oral absorption. The clearance and volume of distribution at steady state in humans are predicted to be 27.3 mL/h/kg and 93.9 mL/kg, respectively. AMG 900 exhibits acceptable PK properties in preclinical species and is predicted to have low clearance in humans. Read more...
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 to the antimitotic drug paclitaxel 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). Read more...
Cell Research	Tumor cells are treated with AMG 900 for 48 hours, washed twice with complete media, and cells are replated at a density of 5000 cells per well in drug-free complete media. Cells are grown until the DMSO control wells are confluent. Cells are stained with crystal violet dye, washed with distilled water, and imaged using a digital scanner.(Only for Reference) Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

Aurora Kinase, Aurora C, AuroraKinase, Aurora A, Aurora B, AMG900, AMG-900, AMG 900, Inhibitor, inhibit, p38MAPK, p38α, p38 MAPK, Tyk2, TyrosineKinases, Tyrosine Kinases

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

24856041 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

AMG 900 (orb1300819)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	>98% (HPLC)
CAS Number:	945595-80-2
MW:	503.6
Formula:	C₂₈H₂₁N₇OS

AMG 900

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

AMG-900 [orb1223553]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

AMG 900 (orb1300819)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors