2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. ALK-IN-23

ALK-IN-23 是一种有效的 ALK 抑制剂，对 ALKWT、ALKL1196M 和 ALKG1202R 的 IC50 分别为 1.6 nM、0.71 nM 和 1.3 nM。ALK-IN-23 可将细胞阻滞在 G2 期，并诱导细胞凋亡 (apoptosis)。ALK-IN-23 在体外抑制癌细胞迁移和集落形成。ALK-IN-23 在 H2228 异种移植裸鼠模型中表现出抗良好的肿瘤活性与低毒性。

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ALK-IN-23 Chemical Structure

ALK-IN-23 Chemical Structure

CAS No. : 3033549-18-4

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ALK-IN-23 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

ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALKWT, ALKL1196M and ALKG1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity[1].

IC50 & Target

IC50: 1.6 nM (ALKWT), 0.71 nM (ALKL1196M), 1.3 nM (ALKG1202R)[1]
体外研究
(In Vitro)

ALK-IN-23 (compound Y28) (0-5 μM; 72h) has highly inhibitory activity against H3122, H2228, Karpas299 and A549[1].
ALK-IN-23 (25-100 nM; 3 days) clearly reduces the number of H2228 cell colonies, and almost completely abolishes the formation of colonies at 100 nM[1].
ALK-IN-23 (100-200 nM; 48 h) facilitates the apoptosis of H2228 cells[1].
ALK-IN-23 (5-10 nM; 24 and 48 h) is effective to block the migration of most cells at a dose of 10 nM[1].
ALK-IN-23 (25-100 nM; overnight) significantly increases the percentage of cells in the G2 phase[1].

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

ALK-IN-23 相关抗体:

Cell Proliferation Assay[1]

Cell Line: H3122, H2228, Karpas299 and A549
Concentration: 0-5 μM
Incubation Time: 72 h
Result: Exhibited highly inhibitory activity against H3122, H2228, Karpas299 and A549 with IC50s of 12 nM, 17 nM, 15 nM and 1.33 μM.

Apoptosis Analysis[1]

Cell Line: H2228 cells
Concentration: 100 nM, 200 nM
Incubation Time: 48 h
Result: Facilitated the apoptosis of H2228 cells in a dose dependent manner and exhibited a more pro-apoptotic effect than that of Ceritinib (HY-15656).

Cell Migration Assay [1]

Cell Line: H2228 cells
Concentration: 5 nM and 10 nM
Incubation Time: 24 and 48 h
Result: Blocked the migration of most cells at a dose of 10 nM (migration rate: 24 h 2.31%, 48 h: 5.01%).

Cell Cycle Analysis[1]

Cell Line: H2228 cells
Concentration: 25 nM, 50 nM, 100 nM
Incubation Time: Overnight
Result: Significantly increased the percentage of cells in the G2 phase from 11.28% to 73.23% in a dramatic dose-dependent manner, accompanied by a resultant loss of G1-and S-phase populations.
体内研究
(In Vivo)

ALK-IN-23 notes a moderate half-life of 16.3 min and a high intrinsic liver clearance of 152.9 mL/min/kg in rats[1].
ALK-IN-23 (25 and 50 mg/kg; IG; once every 2 days; for 14 days) exhibited gentle antitumor efficacy and no significant weight loss in H2228 xenograft mice model[1].

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

Animal Model: Female BALB/c nude mice (5×106 cells H2228 cells suspended in serum-free media were injected into the flanks)[1]
Dosage: 25 and 50 mg/kg
Administration: IG; once every 2 days; for 14 days
Result: Presented moderate antitumor efficacy with the tumor growth inhibition (TGI) of 70.46% at 50 mg/kg.
Possessed gentle antitumor efficacy and exhibited no significant weight loss.
分子量

569.08

Formula

C26H29ClN8O3S
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

ALK-IN-23 相关分类

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  • 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:

ALK-IN-233033549-18-4Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246anticancerH3122H2228Karpas299A549BALB/c nude micexenograftG2 phaseInhibitorinhibitorinhibit

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目录号：
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