Cat. No.: HY-W016889

CFL-137

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CFL-137 is a potent KRas^G12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer.

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Pureté: 99.92%
CAS No.: 708-06-5
Formule: C₁₁H₈O₂
Masse moléculaire:172.18

Stockage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

CFL-137 Chemical Structure

CAS No.: 708-06-5

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Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

CFL-137 is a potent KRas^G12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer^[1].

IC₅₀ & Target^[1]

KRAS(G12C)

Voir tous les produits spécifiques à Isoform Ras :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	43.3 μM Compound: CFL-137	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	46.9 μM Compound: CFL-137	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	10.8 μM Compound: CFL-137	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	32.4 μM Compound: CFL-137	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	24.5 μM Compound: CFL-137	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	25 μM Compound: CFL-137	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	11.4 μM Compound: CFL-137	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	12.3 μM Compound: CFL-137	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	27.6 μM Compound: CFL-137	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]
Sf21	IC₅₀	9732 nM Compound: 2, A-I06	Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay	[PMID: 24749861]
SW1573	IC₅₀	24.2 μM Compound: CFL-137	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	44.5 μM Compound: CFL-137	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-137 (72 h) shows an antiproliferative effect with IC₅₀s of 11.4, 24.2, 24.5, 12.3, 43.3, 44.5, 27.63, 32.4, 46.9, 26.2, 25.0, 10.8, 66.2 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-137 (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-137 in NOD-SCID female mice^[1].

PK parameters	CFL-137
C_max (ng/mL)	27,366 ± 13,221
T_max (h)	0.25
AUC_t (ng/mL*h)	28,307 ± 6375
t_1/2 (h)	4.0 ± 0.2
V_d (mL)	63.6 ± 13.6
CL(mL/h)	11.0 ± 2.8

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 32.5%.

Chemical Information

CAS No. 708-06-5
Appearance Solid
Masse moléculaire 172.18
Formule C₁₁H₈O₂
Color Light yellow to brown
SMILES

O=CC1=C2C=CC=CC2=CC=C1O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (580.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

5.8079 mL

29.0394 mL

58.0788 mL

5 mM

1.1616 mL

5.8079 mL

11.6158 mL

10 mM

0.5808 mL

2.9039 mL

5.8079 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 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)
Instruction de manipulation (2659 KB)

Références

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	5.8079 mL	29.0394 mL	58.0788 mL	145.1969 mL
	5 mM	1.1616 mL	5.8079 mL	11.6158 mL	29.0394 mL
	10 mM	0.5808 mL	2.9039 mL	5.8079 mL	14.5197 mL
	15 mM	0.3872 mL	1.9360 mL	3.8719 mL	9.6798 mL
	20 mM	0.2904 mL	1.4520 mL	2.9039 mL	7.2598 mL
	25 mM	0.2323 mL	1.1616 mL	2.3232 mL	5.8079 mL
	30 mM	0.1936 mL	0.9680 mL	1.9360 mL	4.8399 mL
	40 mM	0.1452 mL	0.7260 mL	1.4520 mL	3.6299 mL
	50 mM	0.1162 mL	0.5808 mL	1.1616 mL	2.9039 mL
	60 mM	0.0968 mL	0.4840 mL	0.9680 mL	2.4199 mL
	80 mM	0.0726 mL	0.3630 mL	0.7260 mL	1.8150 mL
	100 mM	0.0581 mL	0.2904 mL	0.5808 mL	1.4520 mL

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CFL-137

MCE Bioactive Compound Library

KRAS Targeted Compound Library

Covalent Fragment Library

Lysine Focused Covalent Fragment Library

Multifunctional Covalent Fragment Library

Voir tous les produits spécifiques à Isoform Ras

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CFL-137

MCE Bioactive Compound Library

KRAS Targeted Compound Library

Covalent Fragment Library

Lysine Focused Covalent Fragment Library

Multifunctional Covalent Fragment Library

Voir tous les produits spécifiques à Isoform Ras

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CFL-137 Related Classifications

HY-W016889 Related Classifications