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YHO-13351 

Cat. No. M28213
YHO-13351  Structure
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Biological Activity

YHO-13351 is the precursor of YHO-13177, which is a potent and specific inhibitor of BCRP.

Chemical Information
Molecular Weight 579.73
Formula C27H37N3O7S2
CAS Number 1346753-00-1
Form Solid
Solubility (25°C) DMSO ≥ 38 mg/mL
Storage 4°C, dry, sealed
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] Rishil J Kathawala, et al. Cancers (Basel). ABCG2 Overexpression Contributes to Pevonedistat Resistance

[2] Chien-Hsing Chang, et al. Mol Cancer Ther. Combining ABCG2 Inhibitors with IMMU-132, an Anti-Trop-2 Antibody Conjugate of SN-38, Overcomes Resistance to SN-38 in Breast and Gastric Cancers

[3] Yoshiyuki Shishido, et al. Anticancer Res. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan

[4] Ryuta Yamazaki, et al. Mol Cancer Ther. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo

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Keywords: YHO-13351  supplier, BCRP/ABCG2/MXR/ABCP, inhibitors, activators


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