2. Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. ROS Kinase p38 MAPK ERK Apoptosis
  4. SMU-037

SMU-037 是一种口服有效的选择性 ROS1 抑制剂，其作用强效 (IC₅₀ = 6.8 nM)，且能穿透血脑屏障。SMU-037 对 ALK 的选择性约为 25 倍，且对 G2032R 耐药突变表现出卓越的敏感性。SMU-037 能够抑制 ROS1 及其下游 MAPK-ERK 信号通路的磷酸化，进而引起细胞周期阻滞与细胞凋亡 (apoptosis)。SMU-037 在皮下移植瘤和颅内转移瘤小鼠模型中均能抑制肿瘤生长。SMU-037 可用于非小细胞肺癌 (NSCLC) 的相关研究。

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SMU-037

SMU-037 Chemical Structure

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SMU-037 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research[1].

体外研究
(In Vitro)

SMU-037 (compound 9y) 对 A549 (IC50 = 0.9 μM)、HCC-78 (IC50 = 1.1 μM) 和 NCI-H3122 (IC50 = 1.1 μM) 细胞均表现出显著的活性，并且对 Ba/F3 ROS1G2032R 和 Ba/F3 ROS1L2026R 细胞的抑制作用也十分显著，IC50 值分别为 8.9 nM 和 32.0 nM[1]。
SMU-037 (0.001-3 μM，8 小时) 能以剂量依赖的方式减弱多种 Ba/F3 和 A549 细胞中 ROS1 及其下游关键信号通路 MAPK-ERK 的磷酸化[1]。
SMU-037 (0-100 nM, 48 小时) 可引起细胞周期阻滞 (在 ROS1WT 细胞中阻滞于 G0/G1 期，在 ROS1G2032R 细胞中阻滞于 G2/M 期)，并诱导 Ba/F3-ROS1WT 和 Ba/F3-ROS1G2032R 细胞凋亡[1]。

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

SMU-037 相关抗体:

Western Blot Analysis[1]

Cell Line: Ba/F3-ROS1WT, Ba/F3-ROS1G2032R, Ba/F3-ROS1L2026M and A549-ROS1G2032R cells
Concentration: 1, 10, 100, and 10000 nM, 0.1, 0.3, 1 and 3 μM
Incubation Time: 8 h
Result: Exhibited remarkable inhibitory effects on ROS1G2032R phosphorylation at the concentration of 1000 nM.
Slightly inhibited the downstream MAPK-ERK signaling pathway at the concentration of 1000 nM, with efficacy comparable to Cabozantinib (HY-13016).
Led to attenuated phosphorylation of ROS1 and the key downstream MAPK-ERK signaling pathway in a dose-dependent manner in Ba/F3-ROS1WT and Ba/F3-ROS1L2026M cells, comparable to Crizotinib (HY-50878).
Exhibited a marked suppression of ROS1 phosphorylation at a concentration of 1 μM in A549-ROS1G2032R cells.

Cell Cycle Analysis[1]

Cell Line: Ba/F3-ROS1WT and Ba/F3-ROS1G2032R cells
Concentration: 0, 10, 30, and 100 nM
Incubation Time: 48 h
Result: Significantly increased the percentage of ROS1WT cells in the G0/G1 phase.
Caused a predominant G2/M phase accumulation in ROS1G2032R cells.
The G0/G1 phase of ROS1G2032R cells increased from 57.10 % (control) to 60.71 %, 72.97 %, and 85.28 %, respectively.
The G2/M phase of ROS1G2032R cells increased from 6.14 % (control) to 6.98 %, 14.42 %, and 27.16 %, respectively.

Apoptosis Analysis[1]

Cell Line: Ba/F3-ROS1WT and Ba/F3-ROS1G2032R cells
Concentration: 0, 10, 30, and 100 nM
Incubation Time: 48 h
Result: Induced a dose-dependent increase in apoptosis.
Apoptotic rates in ROS1WT cells rose from 13.12 % (control) to 16.95 %, 31.50 %, and 91.87 %.
Apoptotic rates in ROS1G2032R cells increased from 19.85 % (control) to 20.46 %, 28.03 %, and 54.60 %.
体内研究
(In Vivo)

SMU-037 (15、30 和 60 mg/kg，灌胃，每日一次，持续 14 天) 在异种移植和脑转移小鼠模型中显示出强大的肿瘤生长抑制作用[1]。

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

Animal Model: Male Balb/c nude mice (16-20 g) injected with Ba/F3 CD74-ROS1G2032R cells[1]
Dosage: 15, 30 and 60 mg/kg
Administration: i.g., q.d. for 14 days
Result: Effectively suppressed Ba/F3 tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) values of 118, 140, and 156 %, respectively.
Showed no significant body weight reduction and no morphological changes or side effects in heart, liver and kidney.
Significantly inhibited ROS1 phosphorylation in tumor tissue, demonstrating its on-target effect in vivo.
Induced prominent alterations in the morphological characteristics of tumor cells, including cellular contraction, agglutination, and marginalization of nuclear chromatin.
Significantly reduced expression level of the Ki-67 protein, indicating strong anti-proliferative activity.
Animal Model: Male Balb/c nude mice (16-20 g) injected with A549-ROS1G2032R cells[1]
Dosage: 15, 30 and 60 mg/kg
Administration: i.g., q.d. for 14 days
Result: Demonstrated significant tumor regression at doses of 30 mg/kg and 60 mg/kg, comparable to the positive control Lorlatinib (HY-12215, 30 mg/kg).
Animal Model: Male Balb/c nude mice (16-20 g) injected with luciferase-transduced A549-ROS1G2032R cells[1]
Dosage: 30 and 60 mg/kg
Administration: i.g., q.d. for 14 days
Result: Prominently reduced tumor load (as measured using photon flux) in the brain without obvious body weight loss.
Could penetrate blood-brain barrier.
分子量

523.02

Formula

C29H29ClF2N4O
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

SMU-037 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:

SMU-037SMU037SMU 037ROS Kinasep38 MAPKERKApoptosisExtracellular signal regulated kinasesA549-ROS1G2032RBa/F3-ROS1G2032RROS1ALKHCC827A549NCI-H3122NSCLCMAPK-ERKintracranialInhibitorinhibitorinhibit

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目录号：
HY-178391
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