2. MAPK/ERK Pathway GPCR/G Protein Stem Cell/Wnt Apoptosis
  3. SOS1 Ras p38 MAPK ERK MEK Apoptosis
  4. SL43

SL43 是一种具有口服活性的强效的 SOS1 抑制剂，其 Kd 值为 0.16 μM。SL43 可破坏 SOS1-KRAS 相互作用，抑制 SOS1 介导的 KRAS 突变体核苷酸交换，并阻断 RAS-MAPK 信号通路。SL43 对 KRAS 突变癌细胞具有抗增殖活性，可诱导早期细胞凋亡 (apoptosis) 和 G1 期细胞周期阻滞，同时降低磷酸化 MEK 和 ERK 的水平。SL43 可抑制结直肠癌异种移植模型中的肿瘤生长。

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SL43

SL43 Chemical Structure

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SL43 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

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K-Ras H-Ras N-Ras Ras

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SL43 is an orally active and potent SOS1 inhibitor with a Kd of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model[1].

IC50 & Target[1]

K-RAS

 

体外研究
(In Vitro)

SL43 与 SOScat 结合的 Kd 值为 0.16 μM，表明其对 SOS1 催化结构域具有高亲和力[1]。
SL43 可强效破坏 SOS1-KRASG12C 相互作用，其 IC50 为 13.0 nM[1]。
SL43 优先抑制 SOS1 介导的 KRASG12C、KRASG12V 和 KRASG12D 突变体的核苷酸交换，其 IC50 值为 13.4-29.1 nM，而对 KRASWT 的抑制作用较弱 (IC50 = 95.8 nM)[1]。
SL43 (120 h) 可强效且选择性地抑制 KRAS 突变型结直肠癌细胞系的增殖 (IC50 = 0.028-0.238 μM)，对 KRAS 野生型结直肠癌细胞系的选择性超过 100 倍 (IC50 = 2.495-4.520 μM)[1]。
SL43 (10-40 nM; 72 h) 可剂量依赖性地抑制携带 KRAS 突变的 SW620 和 HCT116 结直肠癌细胞系的集落形成[1]。
SL43 (200-800 nM；48 h) 可剂量依赖性地诱导 SW620 和 HCT116 KRAS 突变结直肠癌细胞系发生早期凋亡和 G1 期细胞周期阻滞[1]。
SL43 (50-200 nM；48 h) 可通过降低磷酸化 MEK 和 ERK 水平，以剂量依赖方式抑制 SW620 和 HCT116 KRASG12D/G13D 结直肠癌细胞系中的 RAS-MAPK 信号通路[1]。

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

SL43 相关抗体:

Apoptosis Analysis[1]

Cell Line: KRAS-mutant CRC cell lines (SW620/G12V, HCT116/G13D)
Concentration: 200, 400, 800 nM
Incubation Time: 48 h
Result: Significantly increased the proportion of early apoptotic cells, with high-concentration groups reaching 35.47% in SW620 cells and 25.97% in HCT116 cells.

Cell Cycle Analysis[1]

Cell Line: KRAS-mutant CRC cell lines (SW620/G12V, HCT116/G13D)
Concentration: 200, 400, 800 nM
Incubation Time: 48 h
Result: Induced dose-dependent G1 phase cell cycle arrest, with the G1 population increasing from 64.13% to 78.04% in SW620 cells and from 35.34% to 57.59% in HCT116 cells.

Western Blot Analysis[1]

Cell Line: KRAS-mutant CRC cell lines (SW620/G12V, HCT116/G13D)
Concentration: 50, 100, 200 nM
Incubation Time: 48 h
Result: Led to a concentration-dependent decrease in p-MEK and p-ERK levels in both SW620 and HCT116 cells.
Left total MEK and ERK expression unaltered.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t Tmax T1/2 Cmax F
Mice[1] 20 mg/kg i.v. 6504.1 ng·h/mL 0.1 h 4.2 h 3649.1 ng/mL /
Mice[1] 20 mg/kg p.o. 3697.2 ng·h/mL 2.0 h 4.6 h 468.2 ng/mL 56.8 %
体内研究
(In Vivo)

SL43 (20-40 mg/kg；灌胃；每日一次；连续 18 天) 在 KRAS 突变结直肠癌异种移植模型中展现出强效的剂量依赖性抗肿瘤功效，在 40 mg/kg 剂量下达到 74.9% 的最大 TGI，且未检测到全身毒性[1]。
SL43 (400-800 mg/kg；口服；单次给药) 在 BALB/c 小鼠中具有良好的安全性，其估算的口服半数致死剂量 (LD50) 超过 800 mg/kg[1]。

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

Animal Model: Colorectal cancer BALB/c nude mice (female, 6-8 weeks old, 20-22 g, subcutaneous inoculation of HCT116 KRASG13D cells)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: p.o.; daily; 18 days
Result: Produced a tumor growth inhibition (TGI) rate of 57.2% at 20 mg/kg.
Produced a tumor growth inhibition (TGI) rate of 74.9% at 40 mg/kg.
Induced no significant body weight loss or observable histological alterations in major organs (heart, liver, spleen, lungs, kidneys) at either dose.
分子量

449.03

Formula

C27H33ClN4
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

SL43 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:

SL43SL 43SL-43SOS1Rasp38 MAPKERKMEKApoptosisRas/Rac guanine nucleotide exchange factor 1Extracellular signal regulated kinasesMitogen-activated protein kinase kinaseMAPKKMAP2Kcolorectal cancer xenograft modelKRAS mutantsKRASG12CKRAScolorectal cancer cellsKRASG12VmiceKRASG12DSOScatInhibitorinhibitorinhibit

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