2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. WS-691

WS-691 是一种具有口服活性的、选择性 ABCB1 调节剂。WS-691 可以通过直接与 ABCB1 结合来选择性地稳定 ABCB1。WS-691 抑制 ABCB1 的外排功能，并激活 ABCB1 ATPase 活性。WS-691 可提高细胞内 Paclitaxel (HY-B0015) 水平，并在过表达 ABCB1 的癌细胞中降低所需的 Paclitaxel 剂量。WS-691 提高结肠癌细胞对 Paclitaxel 的敏感性。

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WS-691

WS-691 Chemical Structure

CAS No. : 2035417-32-2

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WS-691 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

WS-691 is an orally active, selective ABCB1 modulator. WS-691 selectively stabilizes ABCB1 via direct binding to ABCB1. WS-691 inhibits the efflux function of ABCB1 and activates ABCB1 ATPase activity. WS-691 elevates intracellular Paclitaxel (HY-B0015) levels and reduces the required dose of Paclitaxel in cancer cells overexpressing ABCB1. WS-691 increases the sensitivity of colon cancer cells to Paclitaxel[1][2].

体外研究
(In Vitro)

WS-691 (20 μM) 在 ABCB1 过表达的耐紫杉醇癌细胞中将紫杉醇的 IC50 从 4.23 μM 降至 0.022 μM，且单独使用时无细胞毒性[1]。
WS-691 (0-40 μM; 20 min) 可将 ABCB1 的 ATPase 活性刺激至基础活性的 2.5 倍[2]。

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

WS-691 相关抗体:
体内研究
(In Vivo)

WS-691 (20 mg/kg；灌胃；每日一次；连续 21 天) 可在 SW620/Ad300 结直肠癌异种移植模型中显著增强 Paclitaxel 的抗肿瘤效果，且未产生可观察到的肝毒性[2]。

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

Animal Model: BALB/c nude (male, 5-6 weeks old, 15-17 g, subcutaneous inoculation of SW620/Ad300 cells)[2]
Dosage: 20 mg/kg (single agent); 20 mg/kg (in combination with paclitaxel 5 mg/kg)
Administration: i.g.; daily; 21 days;
Result: Showed little effect on tumor growth compared to vehicle group when used as a single agent.
Significantly reduced tumor volume and tumor weight compared to paclitaxel alone, paclitaxel plus verapamil, or vehicle group when combined with paclitaxel.
Induced more tumor cell death (evident as nuclear pyknosis in HE staining) and higher levels of tumor cell apoptosis (evident as bright green staining in TUNEL assays) compared to single-agent and control groups when combined with paclitaxel.
Caused no obvious liver injury when used alone or in combination with paclitaxel.
分子量

405.45

Formula

C20H16FN7S
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

WS-691 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

WS-6912035417-32-2WS691WS 691P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243CYP3A4colorectal cancer xenograft modelhuman liver microsomesSW620/Ad300 cell lysatesABCC1ABCB1-overexpressed cancer cellsmultidrug-resistant cancerpaclitaxelpaclitaxel-resistant cancer cellsInhibitorinhibitorinhibit

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HY-182253
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