1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. CFL-120

CFL-120 is a potent KRasG12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer.

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

CFL-120

CFL-120 Chemical Structure

CAS No. : 18711-15-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

CFL-120 is a potent KRasG12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer[1].

IC50 & Target[1]

KRAS(G12C)

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
44.4 μM
Compound: CFL-120
Antiproliferative activity against human A549 cells harboring homozygous KRAS G12S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring homozygous KRAS G12S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
BXPC-3 IC50
13.1 μM
Compound: CFL-120
Antiproliferative activity against human BXPC-3 cells harboring wild type KRAS assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BXPC-3 cells harboring wild type KRAS assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
HUVEC IC50
24.4 μM
Compound: CFL-120
Cytotoxicity against HUVEC cells immortalized with TERT assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against HUVEC cells immortalized with TERT assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
MIA PaCa-2 IC50
13.7 μM
Compound: CFL-120
Antiproliferative activity against human MIA PaCa-2 cells harboring homozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MIA PaCa-2 cells harboring homozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
MRC5 IC50
47.9 μM
Compound: CFL-120
Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
NCI-H1792 IC50
11 μM
Compound: CFL-120
Antiproliferative activity against human NCI-H1792 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1792 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
NCI-H358 IC50
16.9 μM
Compound: CFL-120
Antiproliferative activity against human NCI-H358 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H358 cells harboring heterozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
PANC-1 IC50
38 μM
Compound: CFL-120
Antiproliferative activity against human PANC-1 cells harboring heterozygous KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PANC-1 cells harboring heterozygous KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
SW1573 IC50
23.6 μM
Compound: CFL-120
Antiproliferative activity against human SW1573 cells harboring homozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW1573 cells harboring homozygous KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
SW480 IC50
14.8 μM
Compound: CFL-120
Antiproliferative activity against human SW480 cells harboring homozygous KRAS G12V mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells harboring homozygous KRAS G12V mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36842271]
In Vitro

CFL-120 (72 h) shows an antiproliferative effect with IC50s of 11.0, 23.6, 13.7, 16.9, 44.4, 14.8, 38.0, 30.0, 13.1, 9.8, 47.9, 24.4, 42.7 µM for H1792, SW1573, MiaPaca2, H358, A549, SW480, PANC-1, LCLC-103H, BxPC3, HCA-7, MRC-5, HUVEC-TERT, CCD-986Sk cells, respectively[1].

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

In Vivo

CFL-120 (5 mg/kg, 5 treatments; 15 mg/kg, 5 treatments; 30 mg/kg, 3 treatments; i.p.) reduces tumor growth in subcutaneous H1792 (KRasG12C mutant) and LCLC-103H (KRasWT) human lung cancer-bearing mice[1].
Pharmacokinetic Parameters of CFL-120 in NOD-SCID female mice[1].

PK parameters CFL-137
Cmax (ng/mL) 337 ± 123
Tmax (h) 0.25
AUCt (ng/mL*h) 169 ± 56
t1/2 (h) 4.4 ± 0.6
Vd (mL) 12,096 ± 4000
CL(mL/h) 1895 ± 539
NOD-SCID female mice, 15 mg/kg IP[1].

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

Animal Model: NOD/SCID female mice (KRasWT (LCLC-103H) or KRasG12C (H1792) tumors)[1]
Dosage: 5 mg/kg, 5 treatments; 15 mg/kg, 5 treatments; 30 mg/kg, 3 treatments
Administration: I.p.
Result: Reduced tumor growth compared to the control group in KRasG12C mutated model for 35.8%.
Molecular Weight

216.02

Formula

C8H3Cl2NO2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C1=C(C=C(C2=C1NC(C2=O)=O)Cl)Cl

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 : 100 mg/mL (462.92 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 4.6292 mL 23.1460 mL 46.2920 mL
5 mM 0.9258 mL 4.6292 mL 9.2584 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.

  • Molarity Calculator

  • Dilution Calculator

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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.0%

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 4.6292 mL 23.1460 mL 46.2920 mL 115.7300 mL
5 mM 0.9258 mL 4.6292 mL 9.2584 mL 23.1460 mL
10 mM 0.4629 mL 2.3146 mL 4.6292 mL 11.5730 mL
15 mM 0.3086 mL 1.5431 mL 3.0861 mL 7.7153 mL
20 mM 0.2315 mL 1.1573 mL 2.3146 mL 5.7865 mL
25 mM 0.1852 mL 0.9258 mL 1.8517 mL 4.6292 mL
30 mM 0.1543 mL 0.7715 mL 1.5431 mL 3.8577 mL
40 mM 0.1157 mL 0.5787 mL 1.1573 mL 2.8933 mL
50 mM 0.0926 mL 0.4629 mL 0.9258 mL 2.3146 mL
60 mM 0.0772 mL 0.3858 mL 0.7715 mL 1.9288 mL
80 mM 0.0579 mL 0.2893 mL 0.5787 mL 1.4466 mL
100 mM 0.0463 mL 0.2315 mL 0.4629 mL 1.1573 mL
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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.

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Product Name:
CFL-120
Cat. No.:
HY-W041315
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