Free shipping on all orders over $ 500

AMG 232

Cat. No. M10374
AMG 232 Structure
Synonym:

Navtemadlin ; KRT-232

Size Price Availability
10mg USD 280  USD280 4-7 Days
25mg USD 620  USD620 4-7 Days
50mg USD 1040  USD1040 4-7 Days
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

AMG 232 is an extremely potent MDM2 inhibitor (SPR KD = 0.045 nM, SJSA-1 EdU IC50 = 9.1 nM), with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model (ED50 = 9.1 mg/kg). AMG 232 (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines. AMG 232 potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC50=10 nM).

AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice. AMG 232 (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo.

*The compound is unstable in solutions, freshly prepared is recommended

Chemical Information
Molecular Weight 568.55
Formula C28H35Cl2NO5S
CAS Number 1352066-68-2
Solubility (25°C) DMSO ≥ 48 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jude Canon, et al. Mol Cancer Ther. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents

[2] Yosup Rew, et al. J Med Chem. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer

[3] Ana Z Gonzalez, et al. J Med Chem. Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction

[4] Daqing Sun, et al. J Med Chem. Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development

Related Mdm2 Products
MMRi64

MMRi64 disrupts Mdm2-MdmX interactions.

MeOIstPyrd

MeOIstPyrd is an anti-skin cancer agent.

MDM2/XIAP-IN-3

MDM2/XIAP-IN-3 is a dual MDM2/XIAP inhibitor.

UNP-6457

UNP-6457 is a potent active MDM2-p53 interaction inhibitor with an IC50 values of 8.9 nM.

YL93

YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively.

  Catalog
Abmole Inhibitor Catalog




Keywords: AMG 232, Navtemadlin ; KRT-232 supplier, Mdm2, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.