1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. Fulzerasib

Fulzerasib  (Synonyms: IBI351; GFH925)

Cat. No.: HY-152848 Purity: 99.60%
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Fulzerasib (GFH925) is an irreversible KRAS G12C inhibitor, has a synergistic anti-cancer effect with cetuximab (HY-P9905)..

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

Fulzerasib Chemical Structure

Fulzerasib Chemical Structure

CAS No. : 2641747-54-6

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Description

Fulzerasib (GFH925) is an irreversible KRAS G12C inhibitor, has a synergistic anti-cancer effect with cetuximab (HY-P9905).[1][2].

IC50 & Target

KRAS(G12C)

 

In Vitro

Fulzerasib covalently inhibits GDP/GTP nucleotide exchange on KRAS G12C (IC50: 29 nM), locking KRAS in its inactive GDP-bound state (RAS-GTP IC50: 74 nM), thereby blocking the KRAS signaling pathway (pERK IC50: 37 nM)[1].
Fulzerasib inhibits the growth of tumor cell lines carrying the KRAS G12C mutation (IC50: 2-20 nM)[1].

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

In Vivo

Fulzerasib shows strong anti-tumor activity in various models, including the pancreatic cancer cell line MIA Paca-2 CDX, human lung adenocarcinoma NCI-H358 CDX, patient-derived xenograft colon adenocarcinoma SW837 CDX, and lung cancer LU2529 PDX[1].

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

Molecular Weight

617.07

Formula

C32H30ClFN6O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C=C)N1CCN2C(C3=C(N4C5=C(C(C)C)N=CC=C5C)N=C(C6=C(O)C=CC=C6F)C(Cl)=C3)=C(N(C)C([C@@]2([H])C1)=O)C4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 116.67 mg/mL (189.07 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 1.6206 mL 8.1028 mL 16.2056 mL
5 mM 0.3241 mL 1.6206 mL 3.2411 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
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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
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 1.6206 mL 8.1028 mL 16.2056 mL 40.5140 mL
5 mM 0.3241 mL 1.6206 mL 3.2411 mL 8.1028 mL
10 mM 0.1621 mL 0.8103 mL 1.6206 mL 4.0514 mL
15 mM 0.1080 mL 0.5402 mL 1.0804 mL 2.7009 mL
20 mM 0.0810 mL 0.4051 mL 0.8103 mL 2.0257 mL
25 mM 0.0648 mL 0.3241 mL 0.6482 mL 1.6206 mL
30 mM 0.0540 mL 0.2701 mL 0.5402 mL 1.3505 mL
40 mM 0.0405 mL 0.2026 mL 0.4051 mL 1.0129 mL
50 mM 0.0324 mL 0.1621 mL 0.3241 mL 0.8103 mL
60 mM 0.0270 mL 0.1350 mL 0.2701 mL 0.6752 mL
80 mM 0.0203 mL 0.1013 mL 0.2026 mL 0.5064 mL
100 mM 0.0162 mL 0.0810 mL 0.1621 mL 0.4051 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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Fulzerasib
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HY-152848
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