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Oncrasin-1

Cat. No. M3756
Oncrasin-1 Structure
Size Price Availability Quantity
10mg USD 108  USD120 In stock
50mg USD 468  USD520 In stock
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Biological Activity

Oncrasin-1 is a proapoptotic agent that induces abnormal nuclear aggregation of PKCι and suppresses RNA transcription. Exhibits antiproliferative effects against various human tumor cell lines with K-Ras mutations (IC50 ≤ 3 μM) with minimal effects on normal epithelial cells and inhibits human xenograft growth by 75% in vivo. Oncrasin-1 induces aggregation of PKCL in the nuclei and is proapoptotic. oncrasin-1 or its active analogues could be a novel class of anticancer agents, which effectively kill K-Ras mutant cancer cells.

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 269.73
Formula C16H12ClNO
CAS Number 75629-57-1
Purity 99.10%
Solubility DMSO 39 mg/mL
Storage at -20°C
References

Analogues and derivatives of oncrasin-1, a novel inhibitor of the C-terminal domain of RNA polymerase II and their antitumor activities.
Wu S, et al. J Med Chem. 2011 Apr 28;54(8):2668-79. PMID: 21443218.

Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1).
Guo W, et al. Mol Cancer Ther. 2009 Feb;8(2):441-8. PMID: 19208825.

Identification of a Small Molecule with Synthetic Lethality for K-Ras and Protein Kinase C Iota.
Guo W, et al. Cancer Res. 2008 Sep 15;68(18):7403-8. PMID: 18794128.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Oncrasin-1 supplier, PKC, inhibitors

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