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  4. CFL-137

CFL-137 is a potent KRasG12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer.

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

CFL-137 Chemical Structure

CFL-137 Chemical Structure

CAS No. : 708-06-5

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Description

CFL-137 is a potent KRasG12C 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)

 

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
Cmax (ng/mL) 27,366 ± 13,221
Tmax (h) 0.25
AUCt (ng/mL*h) 28,307 ± 6375
t1/2 (h) 4.0 ± 0.2
Vd (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%.
Molecular Weight

172.18

Formula

C11H8O2

CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Purity & Documentation

Purity: 99.53%

References
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  • 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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CFL-137
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HY-W016889
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