1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. KRAS inhibitor-9

KRAS inhibitor-9 

Cat. No.: HY-137497
Handling Instructions

KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.

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

KRAS inhibitor-9 Chemical Structure

KRAS inhibitor-9 Chemical Structure

CAS No. : 300809-71-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
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100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Description

KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells[1].

In Vitro

KRAS inhibitor-9 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively[1].
KRAS inhibitor-9 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC50s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours)[1].
KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells[1].
KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway[1].
KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC[1].

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

Cell Viability Assay[1]

Cell Line: H2122 (KRAS G12C), H358 (KRAS G12C) and H460 (KRAS Q61H) cell lines
Concentration: 0, 25, 50, 100 μM
Incubation Time: 24, 48, and 72 hours
Result: Inhibited three NSCLC cell lines in a dose- and time-dependent manner, but not in normal lung fibroblast cell line CCD-19Lu.

Western Blot Analysis[1]

Cell Line: H2122, H358 and H460 cells
Concentration: 0, 25, 50, 100 μM
Incubation Time: 48 hours
Result: Reduces the levels of phosphorylation of CRAF and AKT in a dose-dependent manner in H2122, H358 and H460 cells.

Apoptosis Analysis[1]

Cell Line: H2122, H358, H460 cells
Concentration: 0, 25, 50, 100 μM
Incubation Time: 24-72 hours
Result: Significantly decreased in G0/G1 phase while remarkably increased in G2/M phase after 24 hours and induced a significantly increased apoptosis for 48h in NSCLC cell lines.
Molecular Weight

292.81

Formula

C₁₃H₉ClN₂S₂

CAS No.

300809-71-6

SMILES

NC1=CC=C(SC2=NC3=CC=CC=C3S2)C(Cl)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (853.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4152 mL 17.0759 mL 34.1518 mL
5 mM 0.6830 mL 3.4152 mL 6.8304 mL
10 mM 0.3415 mL 1.7076 mL 3.4152 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (7.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

KRAS inhibitor-9KRAS inhibitor9KRAS inhibitor 9RasApoptosisnon-smallcelllungcancercellscytotoxicityproliferationGTP-KRASmutantH2122H358H460Inhibitorinhibitorinhibit

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KRAS inhibitor-9
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HY-137497
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