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MK8242

Cat. No. M40517
MK8242 Structure
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Biological Activity

MK8242 is a small molecule MDM2 inhibitor that stabilizes the tumor suppressor TP53 and can be used in studies related to acute myeloid leukemia and solid tumors.

Chemical Information
Molecular Weight 838.90
Formula C42H48F6N2O7S
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] Yuan Fang et al. Acta Pharm Sin B. Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives

[2] Guochao Liao et al. Eur J Med Chem. The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy

[3] Andrew J Wagner et al. J Clin Oncol. Phase I Trial of the Human Double Minute 2 Inhibitor MK-8242 in Patients With Advanced Solid Tumors

[4] Farhad Ravandi et al. Leuk Res. A phase I trial of the human double minute 2 inhibitor (MK-8242) in patients with refractory/recurrent acute myelogenous leukemia (AML)

[5] Min H Kang et al. Pediatr Blood Cancer. Initial Testing (Stage 1) of MK-8242-A Novel MDM2 Inhibitor-by the Pediatric Preclinical Testing Program

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  Catalog
Abmole Inhibitor Catalog




Keywords: MK8242 supplier, Mdm2, inhibitors, activators


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