2. GPCR/G Protein MAPK/ERK Pathway Apoptosis PI3K/Akt/mTOR
  3. Ras Apoptosis PI3K Akt p38 MAPK
  4. pan-KRAS-IN-5

pan-KRAS-IN-5 是一种泛 KRAS 翻译抑制剂，靶向作用于 5′-UTR RNA G- 四链体 (rG4s)。pan-KRAS-IN-5 能与 KRAS rG4s 强结合并稳定其活性，抑制 KRAS 翻译，阻断 MAPK 和 PI3K-AKT 通路。pan-KRAS-IN-5 可诱导细胞周期停滞，促进 KRAS 驱动型癌细胞凋亡 (apoptosis)。pan-KRAS-IN-5 可抑制 KRAS 突变异种移植瘤的肿瘤生长和 KRAS 表达，可用于 KRAS 驱动型癌症的研究。

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pan-KRAS-IN-5

pan-KRAS-IN-5 Chemical Structure

CAS No. : 3027172-23-9

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规格 价格 是否有货 数量
1 mg ￥1700
1 - 2 周
5 mg ￥4250
1 - 2 周
10 mg 询价 1 - 2 周
50 mg   询价  
100 mg   询价  

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pan-KRAS-IN-5 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 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
4 μM
Compound: 15a
Cytotoxicity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
HFL1 IC50
> 40 μM
Compound: 15a
Cytotoxicity against human HFL1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human HFL1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
HPAF-II IC50
5.4 μM
Compound: 15a
Cytotoxicity against human HPAF-II cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human HPAF-II cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
LX-2 IC50
> 40 μM
Compound: 15a
Cytotoxicity against human LX2 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human LX2 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
MIA PaCa-2 IC50
33 μM
Compound: 15a
Cytotoxicity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
NCI-H358 IC50
4.8 μM
Compound: 15a
Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
NCM460 IC50
> 40 μM
Compound: 15a
Cytotoxicity against human NCM460 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human NCM460 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
PANC-1 IC50
5.6 μM
Compound: 15a
Cytotoxicity against human PANC-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human PANC-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
PANC-1 IC50
> 40 μM
Compound: 15a
Cytotoxicity against human PANC-1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human PANC-1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
SW-620 IC50
5.1 μM
Compound: 15a
Cytotoxicity against human SW620 cells harboring KRAS G12V mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human SW620 cells harboring KRAS G12V mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
U-87MG ATCC IC50
> 40 μM
Compound: 15a
Cytotoxicity against human U-87 MG cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human U-87 MG cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay
[PMID: 38272464]
体外研究
(In Vitro)

pan-KRAS-IN-5 (compound 15a) 与 KRAS rG4s 强结合，对 utr-z 的 KD 值为 2.3 μM，对 utr-1 的 KD 值为 0.9 μM[1]。
pan-KRAS-IN-5 (24 小时) 选择性杀死 KRAS 驱动型癌细胞，包括 MIA PaCa-2 (IC50 = 3.3 μM)、PANC-1 (IC50 = 5.6 μM)、HPAF-II (IC50 = 5.4 μM)、SW620 (IC50 = 5.1 μM)、HCT116 (IC50 = 4.0 μM) 和 NCI-H358 细胞 (IC50 = 4.8 μM)，但对 KRASWT 胶质母细胞瘤细胞或 KRASWT 正常细胞无明显的细胞毒性[1]。
Pan-KRAS-IN-5 (1.25-5.0 μM，0-48 小时) 可抑制 PANC-1、MIA PaCa-2 和 NCI-H358 细胞中的 KRAS 蛋白表达，且不改变 KRAS mRNA 水平[1]。
pan-KRAS-IN-5 (1.25-5.0 μM，0-24 小时) 以剂量和时间依赖性的方式抑制 MEK、ERK、AKT 和 mTOR 的磷酸化[1]。
pan-KRAS-IN-5 (0.32-1.25 μM，10 天) 可抑制 MIA PaCa-2 细胞的增殖[1]。
pan-KRAS-IN-5 (1.25-5.0 μM，24 小时) 可诱导 MIA PaCa-2 细胞剂量依赖性 G2/M 期阻滞，并诱导 KRAS 突变型 MIA PaCa-2 癌细胞中 caspase 3 的裂解[1]。

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

pan-KRAS-IN-5 相关抗体:

Apoptosis Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 1.25, 2.5, and 5.0 μM
Incubation Time: 24 h
Result: Decreased Caspase-3 and increased CL- Caspase-3 leves in MIA PaCa-2 cells.

Cell Cycle Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 1.25, 2.5, and 5.0 μM
Incubation Time: 24 h
Result: Induced G2/M phase arrest in MIA PaCa-2 cells dose-dependently.

Cell Proliferation Assay[1]

Cell Line: MIA PaCa-2 cells
Concentration: 0.32, 0.63, and 1.25 μM
Incubation Time: 10 days
Result: Almost completely inhibited the proliferation of MIA PaCa-2 cells at the concentration of 1.25 μM.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 1.25, 2.5, and 5.0 μM
Incubation Time: 0, 6, 12, and 24 h
Result: Reduced p-MEK, p-ERK, p-AKT and p-mTOR in MIA PaCa-2 cells in a dose-dependent manner.
Decreased p-MEK, p-ERK, p-AKT and p-mTOR in MIA PaCa-2 cells in a time-dependent manner.
体内研究
(In Vivo)

pan-KRAS-IN-5 (2.5 和 5.0 mg/kg，腹腔注射，每日给药，持续 18 天) 抑制肿瘤生长并降低 KRAS 蛋白表达，但不影响 KRAS 突变 MIA PaCa-2 异种移植模型中的总 KRAS mRNA 水平[1]。

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

Animal Model: Male BALB/C-nu/nu (4 weeks old) subcutaneously injected with MIA PaCa-2 cells[1]
Dosage: 2.5 and 5.0 mg/kg
Administration: i.p., every day for 18 days
Result: Inhibited tumor growth in a dose-dependent manner, with Tumor Growth Inhibition (TGI) of 62.0 % (2.5 mg/ kg) and 70.3 % (5.0 mg/kg).
Revealed no significant body weight loss in mice.
Exhibited no evident signs of toxicity in the anatomized viscera.
分子量

642.55

Formula

C31H36FIN4O2
CAS 号
性状

固体

颜色

Brown to black

运输条件

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

4°C, protect from light, stored under nitrogen

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

纯度 & 产品资料
参考文献

pan-KRAS-IN-5 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:

pan-KRAS-IN-53027172-23-9RasApoptosisPI3KAktp38 MAPKPhosphoinositide 3-kinasePKBProtein kinase BTumorKRAS pan-KRASrG4s MAPK pathwayPI3K-AKT pathway KRAS-Driven Cancer Cellscycle arrest apoptosis MIA PaCa-2 cellspancreatic cancer cellscolorectal cancer cellslung cancer cellsInhibitorinhibitorinhibit

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