1. Membrane Transporter/Ion Channel
  2. BCRP
  3. YHO-13351

YHO-13351 

Cat. No.: HY-12758
Handling Instructions

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

For research use only. We do not sell to patients.

YHO-13351 Chemical Structure

YHO-13351 Chemical Structure

CAS No. : 1346753-00-1

Size Price Stock Quantity
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Other Forms of YHO-13351:

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Description

YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP. IC50 value: Target: BCRP inhibitor in vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38–resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. In contrast, it had no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells and multidrug resistance-related protein 1–mediated doxorubicin resistance in MRP1-transfected human epidermoid cancer KB-3-1 cells. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppressed the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1]. in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models [1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 38 mg/mL (65.55 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7249 mL 8.6247 mL 17.2494 mL
5 mM 0.3450 mL 1.7249 mL 3.4499 mL
10 mM 0.1725 mL 0.8625 mL 1.7249 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

579.73

Formula

C₂₇H₃₇N₃O₇S₂

CAS No.

1346753-00-1

SMILES

N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(OC(CN(CC)CC)=O)CC3)S2.O=S(C)(O)=O

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Room temperature in continental US; may vary elsewhere

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YHO-13351
Cat. No.:
HY-12758
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YHO-13351

Cat. No.: HY-12758