1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    PROTAC
  2. EGFR
    PROTAC
  3. Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3 

Cat. No.: HY-123921 Purity: 99.98%
Handling Instructions

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.

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

Gefitinib-based PROTAC 3 Chemical Structure

Gefitinib-based PROTAC 3 Chemical Structure

CAS No. : 2230821-27-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 565 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

IC50 & Target[1]

EGFR

11.7 nM (DC50, HCC827(exon 19 del) cells)

EGFR

22.3 nM (DC50, H3255 (L858R mutantion) cells)

PROTAC

 

In Vitro

H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM; 24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR[1].

Western Blot Analysis[1]

Cell Line: HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR
Concentration: 100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cells
Incubation Time: 24 hours
Result: Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.
Molecular Weight

934.51

Formula

C₄₇H₅₇ClFN₇O₈S

CAS No.

2230821-27-7

SMILES

O=C([[email protected]]1N(C([[email protected]@H](NC(CCOCCOCCCCCOC2=CC3=C(NC4=CC=C(F)C(Cl)=C4)N=CN=C3C=C2OC)=O)C(C)(C)C)=O)C[[email protected]](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (64.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0701 mL 5.3504 mL 10.7008 mL
5 mM 0.2140 mL 1.0701 mL 2.1402 mL
10 mM 0.1070 mL 0.5350 mL 1.0701 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (1.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (1.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Gefitinib-based PROTAC 3
Cat. No.:
HY-123921
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