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CFM-4 

Cat. No. M29925
CFM-4  Structure
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Biological Activity

CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells.

Chemical Information
Molecular Weight 405.9
Formula C22H16ClN3OS
CAS Number 331458-02-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Ramesh Nimma, et al. Pharmaceutics. Combined Transcriptomic and Proteomic Profiling to Unravel Osimertinib, CARP-1 Functional Mimetic (CFM 4.17) Formulation and Telmisartan Combo Treatment in NSCLC Tumor Xenografts

[2] Jaganathan Venkatesh, et al. Genes Cancer. Novel strategies to target chemoresistant triple-negative breast cancer

[3] Nagavendra Kommineni, et al. Eur J Pharm Biopharm. Role of nano-lipid formulation of CARP-1 mimetic, CFM-4.17 to improve systemic exposure and response in osimertinib resistant non-small cell lung cancer

[4] Vino T Cheriyan, et al. Oncotarget. CARP-1 functional mimetics are novel inhibitors of drug-resistant triple negative breast cancers

[5] G De Sarro, et al. Pharmacol Biochem Behav. Anticonvulsant activity and plasma level of 2,3-benzodiazepin-4-ones (CFMs) in genetically epilepsy-prone rats

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Keywords: CFM-4  supplier, Apoptosis, inhibitors, activators


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