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 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.

For research use only. We do not sell to patients.

pan-KRAS-IN-5

pan-KRAS-IN-5 Chemical Structure

CAS No. : 3027172-23-9

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

pan-KRAS-IN-5 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE pan-KRAS-IN-5

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K-Ras H-Ras N-Ras Ras

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

View All p38 MAPK Isoform Specific Products:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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]
In Vitro

pan-KRAS-IN-5 (compound 15a) strongly binds to KRAS rG4s with KD values of 2.3 μM for utr-z and 0.9 μM for utr-1[1].
pan-KRAS-IN-5 (24 h) selectively kills KRAS-driven cancer cells, including 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), and NCI-H358 cells (IC50 = 4.8 μM), but shows no appreciable cytotoxicity in KRASWT glioblastoma cells or KRASWT normal cells[1].
Pan-KRAS-IN-5 (1.25-5.0 μM, 0-48 h) inhibits KRAS protein expression in PANC-1, MIA PaCa-2, and NCI-H358 cells without altering KRAS mRNA levels[1].
pan-KRAS-IN-5 (1.25-5.0 μM, 0-24 h) dose- and time-dependently inhibits the phosphorylation of MEK, ERK, AKT, and mTOR[1].
pan-KRAS-IN-5 (0.32-1.25 μM, 10 days) inhibits the proliferation of MIA PaCa-2 cells[1].
pan-KRAS-IN-5 (1.25-5.0 μM, 24 h) triggers a dose-dependent G2/M phase arrest in MIA PaCa-2 cells, and induces the cleavage of caspase 3 in KRAS mutant MIA PaCa-2 cancer[1].

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

pan-KRAS-IN-5 Related Antibodies

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.
In Vivo

pan-KRAS-IN-5 (2.5 and 5.0 mg/kg, i.p., every day for 18 days) inhibits tumor growth and reduces KRAS protein expression, but dose not effect total KRAS mRNA levels in a KRAS-mutant MIA PaCa-2 xenograft model[1].

MedChemExpress (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.
Molecular Weight

642.55

Formula

C31H36FIN4O2
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

C[N+]1=C(/C=C/C2=CC3=CC=C(N(CC)CC)C=C3OC2=O)C=CC4=C1C=C(NCCN5CCCC5)C(F)=C4.[I-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (77.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5563 mL 7.7815 mL 15.5630 mL
5 mM 0.3113 mL 1.5563 mL 3.1126 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (1.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (1.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5563 mL 7.7815 mL 15.5630 mL 38.9075 mL
5 mM 0.3113 mL 1.5563 mL 3.1126 mL 7.7815 mL
10 mM 0.1556 mL 0.7781 mL 1.5563 mL 3.8907 mL
15 mM 0.1038 mL 0.5188 mL 1.0375 mL 2.5938 mL
20 mM 0.0778 mL 0.3891 mL 0.7781 mL 1.9454 mL
25 mM 0.0623 mL 0.3113 mL 0.6225 mL 1.5563 mL
30 mM 0.0519 mL 0.2594 mL 0.5188 mL 1.2969 mL
40 mM 0.0389 mL 0.1945 mL 0.3891 mL 0.9727 mL
50 mM 0.0311 mL 0.1556 mL 0.3113 mL 0.7781 mL
60 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6485 mL
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pan-KRAS-IN-5 Related Classifications

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:

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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