2. Protein Tyrosine Kinase/RTK TGF-beta/Smad Stem Cell/Wnt
  3. TAM Receptor Discoidin Domain Receptor TGF-β Receptor Hedgehog
  4. Axl-IN-21

Axl-IN-21 是一种口服有效的选择性 AXL 抑制剂， Kd 为 2.7 nM， IC50 为 4.0 nM。Axl-IN-21 在保持激酶选择性的同时，对多种癌症相关激酶亦表现出较强抑制活性，包括 Mer (Kd = 1.4 nM)、DDR1 (IC50 = 22.2 nM)、HIPK4 (Kd = 11.0 nM) 和 LOK (Kd = 10 nM)。Axl-IN-21 可通过阻断肿瘤相关成纤维细胞来源的 GAS6 所诱导的 AXL/STAT3/ABCG1 信号通路，克服肿瘤微环境驱动的耐药性，从而恢复化疗敏感性并抑制药物外排。Axl-IN-21 在 MDA-MB-231 细胞中能够抑制 TGF-β1 诱导的上皮-间质转化、细胞迁移与侵袭。Axl-IN-21 对非癌细胞未表现出显著毒性。Axl-IN-21 可用于三阴性乳腺癌和胃癌的相关研究。

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Axl-IN-21

Axl-IN-21 Chemical Structure

CAS No. : 1958081-87-2

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Axl-IN-21 相关抗体

Top Publications Citing Use of Products

查看 TAM Receptor 亚型特异性产品:

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Axl Mer Tyro3

查看 Discoidin Domain Receptor 亚型特异性产品:

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DDR1 DDR2

查看 TGF-β Receptor 亚型特异性产品:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer[1] [2] .

IC50 & Target[1]

DDR1

22.2 nM (IC50)

Mer

1.4 nM (Kd)

Axl

4 nM (IC50)

Axl

2.7 nM (Kd)

体外研究
(In Vitro)

Axl-IN-21 (compound 9im) (0.1-0.5 μM) 在 SNU668 和 MKN1 胃癌细胞中，即使在与 CAF 共培养的条件下，也能剂量依赖性地抑制 AXL 磷酸化并逆转上皮-间质转化 (恢复 E-cadherin、降低 N-cadherin 表达)；并通过阻断 CAF 诱导的 AXL 激活及下游信号传导来恢复化疗敏感性，尽管与 CAF 共培养通常会在使用含 5-Fluorouracil (5 FU) (HY-90006) and cisplatin (HY-17394) 的化疗后降低凋亡标志物 (切割的 PARP 和切割的 Caspase-3) 水平[1]。
Axl-IN-21 (0.5-32 μM) 在非癌细胞中表现出比 BGB324 更低的细胞毒性[1]。
Axl-IN-21 (0.1-0.5 μM) 抑制 JAK1/STAT3、PI3K/AKT 和 MEK/ERK 信号通路，并减少在与癌症相关成纤维细胞 (CAF) 共培养的 SNU668 细胞中 CAF 诱导的细胞迁移增强，即使在 CAF 条件培养基或直接共培养存在下也是如此[1]。
Axl-IN-21 (0.5-2 μM) 在与 CAF 共培养和/或化疗药物处理的 SNU668 细胞中抑制 CAF 诱导的 AXL 激活、下游信号传导、GC 细胞迁移和化疗耐药[1]。
Axl-IN-21 (0.1-0.5 μM) 在经重组 GAS6 处理的 AXL 激活的 GC SNU668 细胞中，同时抑制 ABCG1 表达的上调以及 AXL、JAK1/STAT3、PI3K/AKT 和 MEK/ERK 的磷酸化[1]。
Axl-IN-21 在与 CAF 和 5-FU 联合时，能降低 ABCG1 表达并增加切割的 Caspase-3 阳性细胞，表明细胞凋亡增强[1]。
Axl-IN-21 (0.03-3 μM, 6 h) 在 MDA-MB-231 乳腺癌细胞中具有强大的 Axl 激酶抑制能力[2]。
Axl-IN-21 (0.04-5 μM, 96-144 h) 剂量依赖性地抑制 MDA-MB-231 乳腺癌细胞中 TGF-β1 诱导的 Axl 激活[2]。
Axl-IN-21 (0.04-5 μM, 24 h) 抑制 MDA-MB-231 细胞的迁移过程和侵袭能力[2]。

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

Axl-IN-21 相关抗体:

Western Blot Analysis[2]

Cell Line: MDA-MB-231
Concentration: 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 6 h
Result: Inhibited phosphorylation of Axl and downstream signaling (pAkt, pAxl).

Immunofluorescence[2]

Cell Line: MDA-MB-231
Concentration: 0.04, 0.2, 1 and 5μM
Incubation Time: 96 to 144 h
Result: Dose-dependently restored the protein levels of E cadherin and N-cadherin back to the control levels.
Reversed TGF β1-induced expression level changes of E-cadherin (an epithelial marker) and N-cadherin (a meschenchymal marker) EMT markers in MDA-MB-231 cells.

Cell Migration Assay [2]

Cell Line: MDA-MB-231
Concentration: 0.2, 1.0, 5.0 μM
Incubation Time: 24 h
Result: Moderately inhibited the migrating process in MDA-MB-231 cells, suppressing the TGF β1 (10 ng/mL)-induced wound closure by ∼24.2%, ∼50.6%, and ∼58.4% at concentrations of 0.2, 1.0, and 5.0 μM.

Cell Invasion Assay[2]

Cell Line: MDA-MB-231
Concentration: 0.04, 0.2, 1.0, or 5.0 μM
Incubation Time: 24 h
Result: Inhibited cancer cell invasion by 48.5%, 52.1%, 73.5%, and 78.1% at concentration of 0.04, 0.2, 1.0, and 5.0 μM, respectively.
体内研究
(In Vivo)

Axl-IN-21 (compound 9im) (90 mg/kg，口服，每日一次，持续 3 周) 可增加 CAF 混合 SNU668 异种移植瘤中 E-cadherin 的表达，表明其能抑制 CAF 诱导的 AXL 活化及下游信号通路[1]。
Axl-IN-21 (30 或 90 mg/kg，口服，每日一次，持续 21 天）在高转移性 4T1 小鼠乳腺癌细胞的异种移植模型中[2]。

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

Animal Model: SNU668 cells (1×106) with or without induced CFAs (1×106, all cells in 100 μL PBS with 50% Matrigel)-BALB/c nude mice (5 weeks old)[1]
Dosage: 90 mg/kg
Administration: p.o., daily for 3 weeks
Result: Increased E-cadherin expression.
Significantly reduced tumor volume and weight when combined with 5-FU whereas either agent alone had only limited effects.
Animal Model: SNU668 cells (1×106) with or without induced CFAs (1×106, all cells in 100 μL PBS with 50% Matrigel)-BALB/c nude mice (5 weeks old)[1]
Dosage: 90 mg/kg
Administration: p.o., daily for 3 weeks
Result: Increases E-cadherin expression.
Significantly reduced tumor volume and weight when combined with 5-FU whereas either agent alone had only limited effects.
Animal Model: 4T1 cells (0.5 × 106) induced-female BALB/c mice[2]
Dosage: 30 or 90 mg/kg
Administration: p.o., daily for 21 days
Result: Did not show an obvious effect on growth of the primary tumor.
Dose-dependently suppressed both size and number of liver metastases (21.3 and 13.0 in the 30 and 90 mg/kg dosing groups, respectively).
分子量

542.56

Formula

C30H27FN4O5
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

Axl-IN-21 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Axl-IN-211958081-87-2TAM ReceptorDiscoidin Domain ReceptorTGF-β ReceptorHedgehogTyro3AxlMerTransforming growth factor beta receptorsAXLDDR1HIPK4LOKAXL/STAT3/ABCG1TGF-β1triple negative breast cancergastric cancerInhibitorinhibitorinhibit

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