1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. KRAS inhibitor-3

KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf.

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KRAS inhibitor-3 Chemical Structure

KRAS inhibitor-3 Chemical Structure

CAS No. : 900897-56-5

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Based on 1 publication(s) in Google Scholar

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Description

KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf[1].

IC50 & Target[1]

K-Ras WT

0.28 μM (EC50)

KRAS(G12C)

0.63 μM (EC50)

KRas G12D

0.37 μM (EC50)

KRas Q61H

0.74 μM (EC50)

In Vitro

KRAS inhibitor-3 (Compound 11, 0-1 μM, 72 h) inhibits growth of KRAS-expressing lung cancer cells[1].
KRAS inhibitor-3 (0-5 μM) decreases the p-ERK levels in BHK cells stably expressing KRASG12D[1].
KRAS inhibitor-3 (1 μM, 2 h) disrupts interaction of KRAS with Raf[1].
KRAS inhibitor-3 (0-5 μM) decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V[1].

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

Western Blot Analysis[1]

Cell Line: BHK cells stably expressing KRASG12D
Concentration: 0.01, 0.1, 0.5 1, 5 μM
Incubation Time:
Result: Decreased the p-ERK levels at >1μM.
Molecular Weight

413.51

Formula

C25H27N5O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OCCN1CCN(CC1)C2=CC(C3=CC=CC=C3)=NC4=C(C(C)=NN42)C5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (120.92 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 2.4183 mL 12.0916 mL 24.1832 mL
5 mM 0.4837 mL 2.4183 mL 4.8366 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. 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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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. 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 2.4183 mL 12.0916 mL 24.1832 mL 60.4580 mL
5 mM 0.4837 mL 2.4183 mL 4.8366 mL 12.0916 mL
10 mM 0.2418 mL 1.2092 mL 2.4183 mL 6.0458 mL
15 mM 0.1612 mL 0.8061 mL 1.6122 mL 4.0305 mL
20 mM 0.1209 mL 0.6046 mL 1.2092 mL 3.0229 mL
25 mM 0.0967 mL 0.4837 mL 0.9673 mL 2.4183 mL
30 mM 0.0806 mL 0.4031 mL 0.8061 mL 2.0153 mL
40 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5115 mL
50 mM 0.0484 mL 0.2418 mL 0.4837 mL 1.2092 mL
60 mM 0.0403 mL 0.2015 mL 0.4031 mL 1.0076 mL
80 mM 0.0302 mL 0.1511 mL 0.3023 mL 0.7557 mL
100 mM 0.0242 mL 0.1209 mL 0.2418 mL 0.6046 mL
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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.

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KRAS inhibitor-3
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