2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. KRAS inhibitor-9

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.

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KRAS inhibitor-9 Chemical Structure

KRAS inhibitor-9 Chemical Structure

CAS No. : 300809-71-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 229 In-stock
Solution
10 mM * 1 mL in DMSO USD 229 In-stock
Solid
1 mg USD 71 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 450 In-stock
50 mg USD 650 In-stock
100 mg USD 850 In-stock
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Based on 1 publication(s) in Google Scholar

KRAS inhibitor-9 Related Antibodies

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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].

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

KRAS inhibitor-9 Related Antibodies

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.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (853.80 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 3.4152 mL 17.0759 mL 34.1518 mL
5 mM 0.6830 mL 3.4152 mL 6.8304 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4152 mL 17.0759 mL 34.1518 mL 85.3796 mL
5 mM 0.6830 mL 3.4152 mL 6.8304 mL 17.0759 mL
10 mM 0.3415 mL 1.7076 mL 3.4152 mL 8.5380 mL
15 mM 0.2277 mL 1.1384 mL 2.2768 mL 5.6920 mL
20 mM 0.1708 mL 0.8538 mL 1.7076 mL 4.2690 mL
25 mM 0.1366 mL 0.6830 mL 1.3661 mL 3.4152 mL
30 mM 0.1138 mL 0.5692 mL 1.1384 mL 2.8460 mL
40 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1345 mL
50 mM 0.0683 mL 0.3415 mL 0.6830 mL 1.7076 mL
60 mM 0.0569 mL 0.2846 mL 0.5692 mL 1.4230 mL
80 mM 0.0427 mL 0.2134 mL 0.4269 mL 1.0672 mL
100 mM 0.0342 mL 0.1708 mL 0.3415 mL 0.8538 mL
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KRAS inhibitor-9 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:

KRAS inhibitor-9300809-71-6KRAS inhibitor9KRAS inhibitor 9RasApoptosisnon-smallcelllungcancercellscytotoxicityproliferationGTP-KRASmutantH2122H358H460Inhibitorinhibitorinhibit

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