YHO-13351

Cat. No.: HY-12758 Purity: 99.16%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

YHO-13351 is an orally active ABCG2 inhibitor. YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer.

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

YHO-13351 Chemical Structure

CAS No. : 1346753-00-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of YHO-13351:

YHO-13351 free base In-stock

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

YHO-13351 (2 μM; 96 h) potently reverses SN-38 (HY-13704) resistance in ABCG2-overexpressing MDA-MB-231-S120 and NCI-N87-S120 cells, reducing the IC₅₀ value of SN-38 by more than 90%^[1].
YHO-13351 (0.004-0.1 μM) potently inhibits ABCG2-mediated Hoechst 33342 efflux in HeLa cells^[3].
YHO-13351 (0.1 μg/mL; 96 h) sensitizes both HeLa SP cells and non-SP cells to SN-38 in vitro^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:	SN-38-resistant human breast cancer MDA-MB-231-S120 cells, parental MDA-MB-231 cells, SN-38-resistant human gastric cancer NCI-N87-S120 cells, parental NCI-N87 cells
Concentration:	2 μM
Incubation Time:	96 h
Result:	Reduced the SN-38 IC₅₀ for NCI-N87-S120 from 211 nmol/L to 6.4 nmol/L, lowering the resistance factor from 49.1 to 1.6. Reduced the SN-38 IC₅₀ for MDA-MB-231-S120 from 248 nmol/L to 16 nmol/L, lowering the resistance factor from 51.7 to 6.7. Caused minimal change to SN-38 IC₅₀ in parental NCI-N87 (from 4.3 nmol/L to 3.9 nmol/L) and MDA-MB-231 (from 4.8 nmol/L to 2.4 nmol/L) cells.

Cell Cytotoxicity Assay^[3]

Cell Line:	sorted human cervical carcinoma HeLa SP and non-SP cells
Concentration:	0.1 μg/mL
Incubation Time:	96 h
Result:	Reduced the IC₅₀ of SN-38 for both HeLa non-SP and SP cells. Dropped the IC₅₀ for SP cells by 64%.

Parmacokinetics

Species	Dose	Route	F
Mice^[2]	117 mg/kg	p.o.	86.5 %

In Vivo

When administered in combination with IMMU-132 (HY-132254), YHO-13351 (0.6 mg; intravenous injection; single dose) increases the median survival time of mice bearing SN-38-resistant NCI-N87-S120 gastric cancer xenografts by 64% compared with untreated animals^[1].
Combined with Irinotecan (HY-16562), YHO-13351 (100-200 mg/kg; i.p.; once daily on days 1, 5 and 9) dose-dependently prolongs the survival time of mice inoculated with P388/BCRP^[2].
When used in combination with Irinotecan, YHO-13351 (30-200 mg/kg; p.o./i.v.; once daily on days 1, 5 and 9 / at 0 and 4 hours on days 1, 5 and 9 post-Irinotecan administration) dose-dependently enhances the antitumor activity of Irinotecan in HCT116/BCRP xenografts^[2].
Combined with Irinotecan, YHO-13351 (600-1200 mg/kg; p.o.; administered on days 1, 5 and 9) inhibits tumor growth in HeLa non-SP cell and HeLa SP cell xenografts in nude mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NCr athymic nude (nu/nu) mice (female, 4 weeks old)^[1]
Dosage:	0.6 mg
Administration:	i.v.; 3 doses (start of IMMU-132 therapy, 4 hours post-IMMU-132, 24 hours post-IMMU-132)
Result:	Achieved a median mouse survival of 71.5 days, representing a 64% improvement compared to untreated animals. Resulted in 2 out of 10 mice surviving to the end of the study observation period.

Animal Model:	CDF1 (female, 6-week-old)^[2]
Dosage:	100 mg/kg; 200 mg/kg
Administration:	i.p.; once daily on days 1, 5, and 9
Result:	Resulted in a T/C value of 170%. Resulted in a T/C value of 197%.

Animal Model:	BALB/c nude (male, 6-week-old)^[2]
Dosage:	50 mg/kg; 100 mg/kg; 200 mg/kg/30 mg/kg
Administration:	p.o.; once daily on days 1, 5, and 9/i.v.; administered at 0 and 4 hours after irinotecan on days 1, 5, and 9
Result:	Resulted in a significant enhancement of irinotecan's antitumor activity. Resulted in an IR value.

Animal Model:	athymic BALB/c nude (6-week-old, male)^[3]
Dosage:	600 mg/kg total; 1200 mg/kg total, co-administered with irinotecan
Administration:	p.o.; administered on days 1, 5, and 9
Result:	Produced a tumor growth-inhibitory ratio (IR) of 52.4% at the 600 mg/kg total dose, and 58.1% at the 1200 mg/kg total dose. Maintained the SP cell ratio in non-SP-derived tumors below 0.2% with both doses.\nProduced a tumor growth-inhibitory ratio (IR) of 61.4% at the 600 mg/kg total dose, and 66.8% at the 1200 mg/kg total dose. Dose-dependently inhibited the irinotecan monotherapy-induced increase in SP cell ratio, reducing the ratio to below 0.2% at both doses, matching the SP cell ratio in non-SP-derived tumors.

Molecular Weight

579.73

Formula

C₂₇H₃₇N₃O₇S₂

CAS No.

1346753-00-1

Appearance

Solid

Color

Yellow to orange

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (344.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.62 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.62 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.16%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (252 KB) HNMR (148 KB) RP-HPLC (170 KB) LCMS (387 KB)

Handling Instructions (2659 KB)

References

[1]. Chang CH, et al. 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. Mol Cancer Ther. 2016;15(8):1910-1919. [Content Brief]

[2]. Yamazaki R, et al. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Mol Cancer Ther. 2011;10(7):1252-1263. [Content Brief]

[3]. Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013;33(4):1379-1386. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7249 mL	8.6247 mL	17.2494 mL	43.1235 mL
	5 mM	0.3450 mL	1.7249 mL	3.4499 mL	8.6247 mL
	10 mM	0.1725 mL	0.8625 mL	1.7249 mL	4.3124 mL
	15 mM	0.1150 mL	0.5750 mL	1.1500 mL	2.8749 mL
	20 mM	0.0862 mL	0.4312 mL	0.8625 mL	2.1562 mL
	25 mM	0.0690 mL	0.3450 mL	0.6900 mL	1.7249 mL
	30 mM	0.0575 mL	0.2875 mL	0.5750 mL	1.4375 mL
	40 mM	0.0431 mL	0.2156 mL	0.4312 mL	1.0781 mL
	50 mM	0.0345 mL	0.1725 mL	0.3450 mL	0.8625 mL
	60 mM	0.0287 mL	0.1437 mL	0.2875 mL	0.7187 mL
	80 mM	0.0216 mL	0.1078 mL	0.2156 mL	0.5390 mL
	100 mM	0.0172 mL	0.0862 mL	0.1725 mL	0.4312 mL

YHO-13351 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YHO-133511346753-00-1YHO13351YHO 13351BCRPBreast cancer resistance proteinABCG2P-glycoproteinNCI-N87-S120 xenograftsHCT116/BCRP xenograftsHeLa cellsbreast cancer resistance proteinBCRP-mediated drug effluxmultidrug resistance-related protein 1cancer stem/initiating-like side population cellsMDA-MB-231-S120 cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *