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Chemical Structure| 945595-80-2 Chemical Structure| 945595-80-2

Structure of AMG 900
CAS No.: 945595-80-2

Chemical Structure| 945595-80-2

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AMG-900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM, and is > 10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.

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Product Details of AMG 900

CAS No. :945595-80-2
Formula : C28H21N7OS
M.W : 503.58
SMILES Code : CC1=CSC(C2=NN=C(NC3=CC=C(OC4=NC=CC=C4C5=NC(N)=NC=C5)C=C3)C6=C2C=CC=C6)=C1
MDL No. :MFCD18633194
InChI Key :IVUGFMLRJOCGAS-UHFFFAOYSA-N
Pubchem ID :24856041

Safety of AMG 900

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Related Pathways of AMG 900

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • Aurora A

    Aurora A, IC50:5 nM

  • Aurora B

    Aurora B, IC50:4 nM

  • Aurora C

    Aurora C, IC50:1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
DU-145 1 nM and 5 nM 12 hours To evaluate the effect of AMG 900 on the expression of phosphorylated aurora A/B/C protein in DU-145 cells, the results showed a dose-dependent decrease in phosphorylated aurora expression at concentrations above 1 nmol/L. PMC4302682
LNCaP 1 nM and 5 nM 12 hours To evaluate the effect of AMG 900 on the expression of phosphorylated aurora A/B/C protein in LNCaP cells, the results showed a dose-dependent decrease in phosphorylated aurora expression at concentrations above 1 nmol/L. PMC4302682
PC3 1 nM and 5 nM 12 hours To evaluate the effect of AMG 900 on the expression of phosphorylated aurora A/B/C protein in PC3 cells, the results showed a dose-dependent decrease in phosphorylated aurora expression at concentrations above 1 nmol/L. PMC4302682
CU-ACC1 50 nM 2 hours, 24 hours, 48 hours and 72 hours The combination of AMG 900 with PNU-74654 was more effective in decreasing cell viability compared to either AMG 900 or PNU-74654 alone. PMC8297658
CU-ACC2 50 nM 2 hours, 24 hours, 48 hours and 72 hours AMG 900 alone showed the best response in decreasing cell viability, and the combination with PNU-74654 did not enhance the effect of AMG 900. PMC8297658
MOLM-13 cells 10 nM 48 hours AMG 900 inhibited p-histone H3, induced polyploidy, accumulation of p53 protein, apoptosis, and cleavage of Bcl-2 protein in MOLM-13 cells PMC6279493
NCI-H295 50 nM 6 hours and 24 hours AMG 900 treatment increased CTNNB1 and MYC expression, suggesting that AMG 900 might play a role in activating the Wnt-beta catenin pathway. PMC8297658
AML cell lines 0.1 μM 72 hours AMG 900 inhibited AML cell growth by inducing polyploidization and/or apoptosis PMC6279493
CHRF-288–11 cells 0.3 μM 72 hours AMG 900 induced polyploidization and expression of megakaryocyte-lineage markers in CHRF-288–11 cells PMC6279493
Jak2V617F mouse bone marrow cells 0.3 μM 72 hours AMG 900 significantly increased polyploidization and expression of CD41/CD42 in Jak2V617F mouse bone marrow cells PMC6279493

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice COLO 205 tumor xenograft model Oral 3.75, 7.5, 15 mg/kg Single dose, assessed after 3 hours To evaluate the inhibition of p-Histone H3 by AMG 900, results showed significant suppression of p-Histone H3 at 15 mg/kg PMC4221688
NSG mice Systemic MOLM-13 xenograft model Oral 22 mg/kg and 12.6 mg/kg 22 mg/kg for 4 consecutive days, 12.6 mg/kg for 7 consecutive days AMG 900 significantly reduced tumor burden and inhibited [18F]FLT uptake in skeletal tissues of mice PMC6279493
Mice DU-145 xenograft model gavage 3.75 mg/kg and 7.5 mg/kg 4 days per week for 4 weeks To evaluate the effect of AMG 900 in combination with vorinostat on tumor growth in the DU-145 xenograft model, the results showed that low-dose AMG 900 in combination with vorinostat significantly inhibited tumor growth, and the effect was similar to that of high-dose AMG 900 alone. PMC4302682

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.93mL

1.99mL

0.99mL

19.86mL

3.97mL

1.99mL

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