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RA190 hydrochloride

Cat. No. M9577
RA190 hydrochloride Structure
Synonym:

RA190 HCl

Size Price Availability Quantity
10mg USD 210  USD210 In stock
25mg USD 320  USD320 In stock
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Biological Activity

RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. RA190 treatment inhibits proteasome function, causing rapid accumulation of polyubiquitinated proteins. RA190 has therapeutic activity in a xenograft model, and with sorafenib exhibited synergetic killing of HCC cells in vitro. In vivo, RA190 administration profoundly reduces growth of multiple myeloma and ovarian cancer xenografts, and oral RA190 treatment retards HPV16+ syngeneic mouse tumor growth, without impacting spontaneous HPV-specific CD8+ T cell responses.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 596.76
Formula C28H23Cl5N2O2
CAS Number 1617495-03-0
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Ruey-Shyang Soong, et al. BMC Cancer. Bis-benzylidine Piperidone RA190 Treatment of Hepatocellular Carcinoma via Binding RPN13 and Inhibiting NF-κB Signaling

[2] Guang-Yang Yu, et al. Cell Physiol Biochem. RA190, a Proteasome Subunit ADRM1 Inhibitor, Suppresses Intrahepatic Cholangiocarcinoma by Inducing NF-KB-Mediated Cell Apoptosis

[3] Ravi K Anchoori, et al. Cancer Cell. A Bis-Benzylidine Piperidone Targeting Proteasome Ubiquitin Receptor RPN13/ADRM1 as a Therapy for Cancer

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Keywords: RA190 hydrochloride, RA190 HCl supplier, Proteasome, inhibitors

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