2. Membrane Transporter/Ion Channel
  3. P-glycoprotein BCRP
  4. WK-X-34

WK-X-34 是一种低毒高效的多药耐药逆转剂。WK-X-34 通过强效抑制 P-糖蛋白 (P-gp, ABCB1) 和乳腺癌耐药蛋白 (BCRP) 的转运功能，显著增加耐药细胞内抗癌药物及放射性示踪剂的积累。WK-X-34 对 MRP 转运体无明显影响。WK-X-34 不仅能恢复多药耐药卵巢癌细胞对化疗的敏感性，还能显著提升 P-gp 阳性异种移植瘤、脑及肠道组织中 99mTc-Sestamibi 的摄取量。WK-X-34 在体外及小鼠体内 (最高 50 mg/kg 剂量) 均表现出极低的毒性和良好的安全性，可用于克服多药耐药卵巢癌的研究。

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WK-X-34

WK-X-34 Chemical Structure

CAS No. : 908859-10-9

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WK-X-34 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

WK-X-34 (10 nM-100 μM; 15 min+180 min) 可强效抑制 A2780/Adr 细胞中 Pgp 介导的外排作用，IC50 为 82.1 nM，且在移除该化合物后，抑制作用可维持 24 h[1]。
WK-X-34 (10 μM; 1 h+0-60 min 99mTc-Sestamibi) 可在 10 μM 浓度下完全抑制 A2780/Adr 细胞中由 Pgp 介导的 99mTc-Sestamibi 外排，IC50 为 417 nM，可将示踪剂的积累水平恢复至 Pgp 阴性 A2780/wt 细胞中的水平[1]。
WK-X-34 (1-1000 μM; 90 min) 可抑制 MCF7/mx 细胞中 BCRP 介导的 Mitoxantrone (HY-13502) 外排，IC50 为 26.5 μM，且不会改变 BCRP 阴性 MCF7 细胞对 Mitoxantrone 的处置[1]。
WK-X-34 (10 nM-10 mM; 72 hr) 在 A2780/Adr 和 A2780/wt 细胞中表现出较低的体外细胞毒性，其 LD50 值远高于其 P-gp 抑制作用的 IC50 浓度[1]。

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

WK-X-34 相关抗体:

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.
体内研究
(In Vivo)

WK-X-34 (20 mg/kg；腹腔注射；单剂量) 可强效抑制体内 Pgp 活性，使过表达 Pgp 的卵巢癌异种移植物中 99mTc-Sestamidium 的蓄积量增加 136%，并提升包括脑和肠道在内的表达 P-gp 的正常组织中放射性示踪剂的摄取量[1]。
WK-X-34 (20-50 mg/kg；腹腔注射，每日 1 次，连续 14 天) 在健康雄性 CD-1 小鼠中具有良好的耐受性，未观察到明显毒性或肝毒性[1]。

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).
分子量

595.70

Formula

C35H37N3O6
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

WK-X-34 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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