Art. -Nr.: HY-W041315

CFL-120

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CFL-120 is a potent KRas^G12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer.

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Reinheit: 98.0%
CAS. Nr.: 18711-15-4
Formel: C₈H₃Cl₂NO₂
Molecular Weight:216.02

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CFL-120 Chemical Structure

CAS. Nr.: 18711-15-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CFL-120 is a potent KRas^G12C 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)

Alle Ras Isoform-spezifische Produkte anzeigen :

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]
LCLC-103H cell line	IC₅₀	30 μM Compound: CFL-120	Antiproliferative activity against human LCLC-103H cells harboring wild type KRAS assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human LCLC-103H cells harboring wild type KRAS 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
C_max (ng/mL)	337 ± 123
T_max (h)	0.25
AUC_t (ng/mL*h)	169 ± 56
t_1/2 (h)	4.4 ± 0.6
V_d (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%.

Chemical Information

CAS. Nr. 18711-15-4
Appearance Solid
Molecular Weight 216.02
Formel C₈H₃Cl₂NO₂
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.6292 mL

23.1460 mL

46.2920 mL

5 mM

0.9258 mL

4.6292 mL

9.2584 mL

10 mM

0.4629 mL

2.3146 mL

4.6292 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 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)

Verweise

[1]. Orgován Z, et al. Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency. Eur J Med Chem. 2023 Mar 15;250:115212. [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

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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CFL-120

Structurally Diverse Fragment Library

MCE Kinase Hinge Binder Fragment Library

Covalent Fragment Library

Multifunctional Covalent Fragment Library

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CFL-120

Structurally Diverse Fragment Library

MCE Kinase Hinge Binder Fragment Library

Covalent Fragment Library

Multifunctional Covalent Fragment Library

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CFL-120 Related Classifications

HY-W041315 Related Classifications