2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) Apoptosis
  4. W23-1006

W23-1006 是一种选择性共价 ALKBH5 抑制剂。W23-1006 与 ALKBH5 C200 残基结合，IC50 值为 3.848 μM。W23-1006 的抑制活性分别比对 FTO 和 ALKBH3 的抑制活性强约 30 倍和 8 倍。W23-1006 可用于研究三阴性乳腺癌 (TNBC)。

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W23-1006

W23-1006 Chemical Structure

CAS No. : 3035498-92-8

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5 mg ￥1350
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10 mg ￥2160
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25 mg ￥4000
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W23-1006 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

W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC)[1].

体外研究
(In Vitro)

W23-1006 (5 μM; 24 h) 显著增加 MDA-MB-231 和 BT549 细胞中的 mA 丰度[1]。
W23-1006 (3.16-31.6 μM; 24 h) 抑制 MDA-MB-231 和 BT549 细胞活力[1]。
W23-1006 (5 μM) 可明显减少 TNBC 细胞定植面积并抑制细胞迁移[1]。
W23-1006 (5-10 μM) 诱导 MDA-MB-231 细胞凋亡并减少 G2/M 期[1]。

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

W23-1006 相关抗体:

RT-PCR[1]

Cell Line: MDA-MB-231 and BT549 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: The mA abundance significantly increased in cells.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 and BT549 cells
Concentration: 3.16 μM, 10 μM, 31.62 μM
Incubation Time: 24 h
Result: Inhibited cell viability of MDA-MB-231 and BT549 with IC50 values of 10.31 μM and 6.338 μM, respectively.
体内研究
(In Vivo)

W23-1006（25 mg/kg；腹膜内注射（i.p.）；每日一次；连续 14 天）在体内对乳腺癌具有抗肿瘤作用[1]。
W23-1006（25 mg/kg；腹膜内注射；每日一次；连续 10 天）可明显抑制 TNBC 肺转移[1]。
W23-1006（单剂量 25 mg/kg；腹膜内注射）显示 t1/2 范围为 0.509 至 0.983 小时，小鼠血浆中的 Cmax（范围为 1715-2108 ng/mL）在 15 分钟内达到[1]。
100 mg/kg 和 250 mg/kg 剂量的 W23-1006（腹腔注射）均未引起昆明小鼠（22-27g）的不良事件或死亡[1]。

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

Animal Model: Immunodefcient female mouse was subcutaneously injected MDA-MB-231 cells[1].
Dosage: 25 mg/kg (5% DMSO, 10% Kolliphor HS 15, and 85% saline)
Administration: Intraperitoneal injection; once daily; for 14 days
Result: Apparently reduced the tumor volume and weight.
Strongly reduced the FN1 and Ki-67 protein expression level.
Animal Model: Immunodefcient female mouse injected MDA-MB-231LMF3 through the tail vein[1].
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; once daily; for 10 days
Result: Inhibited TNBC lung metastasis.
No apparent pathologic abnormality was observed in the HEstaining results of multiple organs, including heart, liver,spleen, lung, and kidney.
There was no signifcant diference in glutamic pyruvic transaminase(ALT) and glutamic oxaloacetic transaminase (AST) levels in mouse serum, did not infuence mice liver function.
分子量

418.20

Formula

C17H12BrN3O5
CAS 号
性状

固体

颜色

Brown to reddish brown

运输条件

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

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

纯度 & 产品资料
参考文献

W23-1006 相关分类

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  • 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:

W23-10063035498-92-8Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALKBH5 inhibitortriple-negative breast cancer (TNBC)induces the apoptosisdecreases the G2/M phaseantitumor efectsInhibitorinhibitorinhibit

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