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Onametostat (JNJ-64619178)

Cat. No. M13371
Onametostat (JNJ-64619178) Structure
Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 660  USD660 In stock
50mg USD 1570  USD1570 In stock
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Quality Control & Documentation
Biological Activity

Onametostat (JNJ-64619178) is a pseudo-irreversible, orally active, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Good pharmacokinetic properties and safety.

Chemical Information
Molecular Weight 483.36
Formula C22H23BrN6O2
CAS Number 2086772-26-9
Solubility (25°C) DMSO ≥ 60 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] Dirk Brehmer, et al. Mol Cancer Ther. Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity

[2] Jujun Zhou, et al. Epigenetics. Repurposing epigenetic inhibitors to target the Clostridioides difficile- specific DNA adenine methyltransferase and sporulation regulator CamA

[3] Kongkai Zhu, et al. J Comput Aided Mol Des. Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity

[4] Hongrui Tao, et al. Chem Pharm Bull (Tokyo). Discovery of Novel PRMT5 Inhibitors by Virtual Screening and Biological Evaluations

[5] Xiao Li, et al. Expert Opin Ther Pat. A patent review of arginine methyltransferase inhibitors (2010-2018)

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