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Cat. No.: HY-13774

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WK-X-34

WK-X-34 is a low-toxicity, highly effective multidrug resistance reversal agent. By potently inhibiting the transport functions of P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP), WK-X-34 significantly increases the intracellular accumulation of anticancer drugs and radiotracers in drug-resistant cells. WK-X-34 exerts no significant effect on MRP transporters. WK-X-34 not only restores the chemosensitivity of multidrug-resistant ovarian cancer cells, but also significantly enhances the uptake of ^99mTc-Sestamibi in P-gp-positive xenograft tumors, brain and intestinal tissues. WK-X-34 exhibits extremely low toxicity and favorable safety profiles both in vitro and in mice (at doses up to 50 mg/kg), and can be used for research on overcoming multidrug resistance in ovarian cancer.

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CAS No.: 908859-10-9
Formule: C₃₅H₃₇N₃O₆
Masse moléculaire:595.70

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

WK-X-34 Chemical Structure

CAS No.: 908859-10-9

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	IC₅₀	8.7 nM Compound: WK-X-34	Reversal of docetaxel resistance in human DU-145 cells transfected with CYP1B1 assessed as decrease in docetaxel IC50 at 5 uM (Rvb = 23.5 +/- 3.04 nM) Reversal of docetaxel resistance in human DU-145 cells transfected with CYP1B1 assessed as decrease in docetaxel IC50 at 5 uM (Rvb = 23.5 +/- 3.04 nM)	[PMID: 39418747]
K562	IC₅₀	19.56 μM Compound: WK-X-34	Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 27073052]
K562/A02	EC₅₀	30.3 nM Compound: W34; WK-X-34	Reversal of adriamycin resistance in human K562/A02 cells incubated for 48 hrs Reversal of adriamycin resistance in human K562/A02 cells incubated for 48 hrs	[PMID: 36708676]
K562/A02	IC₅₀	0.029 μM Compound: W34; WK-X-34	Reversal of multi-drug resistance in human K562/A02 cells assessed as ADR IC50 Reversal of multi-drug resistance in human K562/A02 cells assessed as ADR IC50	[PMID: 36708676]
K562/A02	IC₅₀	50.1 μM Compound: WK-X-34	Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 27073052]
K562/A02	IC₅₀	9.08 μM Compound: W34; WK-X-34	Cytotoxicity against human K562/A02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human K562/A02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36708676]
MCF7	IC₅₀	0.93 μM Compound: 4a	Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining	[PMID: 19932960]
MDCK	IC₅₀	0.86 μM Compound: 4a	Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay	[PMID: 19932960]
SW-620	IC₅₀	0.063 μM Compound: WK-X-34	Reversal of doxorubicin-induced multidrug resistance in human SW620 cells measured after 48 hrs by CCK-8 method Reversal of doxorubicin-induced multidrug resistance in human SW620 cells measured after 48 hrs by CCK-8 method	[PMID: 38389882]
SW620/AD300	IC₅₀	0.223 μM Compound: WK-X-34	Reversal of doxorubicin-induced multidrug resistance in human SW620/AD300 cells measured after 48 hrs by CCK-8 method Reversal of doxorubicin-induced multidrug resistance in human SW620/AD300 cells measured after 48 hrs by CCK-8 method	[PMID: 38389882]

In Vitro

WK-X-34 (10 nM-100 μM; 15 min pre-incubation, 180 min total with daunorubicin) potently inhibits Pgp-mediated efflux in A2780/Adr cells with an IC₅₀ of 82.1 ± 6 nM, and the inhibitory effect persists for 24 hours after removal of the compound^[1].
WK-X-34 (10 μM; 1 hr pre-incubation, 0-60 min ⁹⁹ᵐTc-Sestamibi incubation) completely inhibits Pgp-mediated efflux of ⁹⁹ᵐTc-Sestamibi in A2780/Adr cells at 10 μM, with an IC₅₀ of 417 ± 189.7 nM, restoring tracer accumulation to levels seen in Pgp-negative A2780/wt cells^[1].
WK-X-34 (1-1000 μM; 90 min after mitoxantrone preloading) inhibits BCRP-mediated mitoxantrone efflux in MCF7/mx cells with an IC₅₀ of 26.5 ± 4.6 μM, without altering mitoxantrone handling in BCRP-negative MCF7 cells^[1].
WK-X-34 (10 nM-10 mM; 72 hr) has low in vitro cytotoxicity in A2780/Adr and A2780/wt cells, with LD₅₀ values well above its Pgp inhibitory IC₅₀ concentrations^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

P-gp-overexpressing human ovarian cancer A2780/Adr cells,
P-gp-negative human ovarian cancer A2780/wt cells
Concentration:

10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM, 10 mM
Incubation Time:

72 hr
Result:

Showed low cytotoxicity in both cell lines, with LD₅₀ values of 152 ± 281 μM in A2780/Adr cells and 112 ± 112 μM in A2780/wt cells.

In Vivo

WK-X-34 (20 mg/kg; i.p.; single dose) potently inhibits in vivo Pgp activity, increasing ^99mTc-Sestamidium accumulation by 136% in Pgp-overexpressing ovarian cancer xenografts and enhancing radiotracer uptake in Pgp-expressing normal tissues including brain and intestine^[1].
WK-X-34 (20-50 mg/kg; i.p.; daily; 14 days) is well tolerated in healthy male CD-1 mice, with no observable toxicity or hepatotoxicity^[1].

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

Animal Model:

BalbC nu/nu (5-week-old female, 20-25 g, subcutaneous implantation of human ovarian cancer cells)^[1]
Dosage:

20 mg/kg
Administration:

i.p.; single dose
Result:

Increased 99mTc-Sestamibi AUC_0-4h by 136% in A2780/Adr xenograft tumors, with no significant change in A2780/wt tumors.
Increased 99mTc-Sestamidium accumulation 9-fold in A2780/Adr tumors (0.95% ID/g tissue vs control 0.09% ID/g tissue).
Increased A2780/Adr tumor-to-muscle ratio from 0.05 to 0.45.
Increased 99mTc-Sestamidium AUC_0-4h by 147% in brain and 138% in intestine.
Increased 99mTc-Sestamidium accumulation in heart (10.09% ID/g tissue vs control 5.90% ID/g tissue), liver (11.91% ID/g tissue vs control 5.83% ID/g tissue), muscle (2.58% ID/g tissue vs control 1.63% ID/g tissue), and brain (0.10% ID/g tissue vs control 0.06% ID/g tissue).

Chemical Information

CAS No. 908859-10-9
Masse moléculaire 595.70
Formule C₃₅H₃₇N₃O₆
SMILES

O=C(NC=1C=CC=CC1C(=O)NC2=CC=C(C=C2)CCN3CC4=CC(OC)=C(OC)C=C4CC3)C5=CC=C(OC)C(OC)=C5
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Jekerle V, et al. In vitro and in vivo evaluation of WK-X-34, a novel inhibitor of P-glycoprotein and BCRP, using radio imaging techniques. Int J Cancer. 2006;119(2):414-422. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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