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  5. 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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CFL-137 Related Antibodies

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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)

 

Cellular Effect
Cell Line Type Value Description References
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]
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.

CFL-137 Related Antibodies
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)

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.8079 mL 29.0394 mL 58.0788 mL
5 mM 1.1616 mL 5.8079 mL 11.6158 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 (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.

  • 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
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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: 99.84%

SDS (453 KB)

COA (252 KB) HNMR (124 KB) RP-HPLC (179 KB)

Handling Instructions (2659 KB)
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 (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.

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 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:

CFL-137708-06-5CFL137CFL 137RasH1792LCLC-103Hanticancerantiproliferativelung cancerInhibitorinhibitorinhibit

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