Cat. No.: HY-163299

pan-KRAS-IN-5

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

Purity: 96.70%
CAS No.: 3027172-23-9
Formula: C₃₁H₃₆FIN₄O₂
Molecular Weight:642.55

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)

pan-KRAS-IN-5 Chemical Structure

CAS No.: 3027172-23-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All Ras Isoforms :

All PI3K Isoforms :

All Akt Isoforms :

All p38 MAPK Isoforms :

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	>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]
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]
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 K_D 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 KRAS^WT glioblastoma cells or KRAS^WT 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.

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.

Chemical Information

CAS No. 3027172-23-9
Appearance Solid
Molecular Weight 642.55
Formula C₃₁H₃₆FIN₄O₂
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)

Publications (1)

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Authorea

2025 Dec 11.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5563 mL

7.7815 mL

15.5630 mL

5 mM

0.3113 mL

1.5563 mL

3.1126 mL

10 mM

0.1556 mL

0.7781 mL

1.5563 mL

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.

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.
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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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Mao-Lin Li, et al. Discovery of Novel Coumarin-quinolinium Derivatives as Pan-KRAS Translation Inhibitors by Targeting 5'-UTR RNA G-Quadruplexes. J Med Chem. 2024 Feb 8;67(3):1961-1981. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

pan-KRAS-IN-5

1 Cited Publications

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pan-KRAS-IN-5

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

PI3K/Akt/mTOR Compound Library

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Publications Citing Use of MedChemExpress (MCE) pan-KRAS-IN-5

All Ras Isoforms

All PI3K Isoforms

All Akt Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

pan-KRAS-IN-5 Related Classifications

Cat. No.: HY-163299