2. Membrane Transporter/Ion Channel
  3. P-glycoprotein BCRP
  4. 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.

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

WK-X-34

WK-X-34 Chemical Structure

CAS No. : 908859-10-9

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Description

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[1].

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.

WK-X-34 Related Antibodies

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 AUC0-4h 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 AUC0-4h 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).
Molecular Weight

595.70

Formula

C35H37N3O6
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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WK-X-34 Related Classifications

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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:

WK-X-34908859-10-9P-glycoproteinBCRPP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Breast cancer resistance proteinABCG2multidrug-resistant ovarian cancer cellshuman ovarian cancer cell linesMCF7/mx cellsxenograft tumorsbreast cancer resistance proteinCD-1 miceA2780/Adr cellsInhibitorinhibitorinhibit

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