2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. HX103

HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe. HX103 inhibits EGFR 19 del, EGFR L858R, EGFR wild type and EGFR T790M with IC50s of 1.3, 1.5, 4.0 and 977 nM, respectively. HX103 can be used for quantifying active-EGFR to predict agent sensitivity in NSCLC patients with EGFR-activating mutations.

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HX103 Chemical Structure

HX103 Chemical Structure

CAS No. : 2566466-98-4

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Based on 1 publication(s) in Google Scholar

HX103 Related Antibodies

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Description

HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe. HX103 inhibits EGFR 19 del, EGFR L858R, EGFR wild type and EGFR T790M with IC50s of 1.3, 1.5, 4.0 and 977 nM, respectively. HX103 can be used for quantifying active-EGFR to predict agent sensitivity in NSCLC patients with EGFR-activating mutations[1].

IC50 & Target[1]

EGFRdel19

1.3 nM (IC50)

EGFRL858R

1.5 nM (IC50)

EGFRWT

4.0 nM (IC50)

EGFRT790M

977 nM (IC50)

In Vitro

HX103 gives remarkable fluorescence enhancement in acetonitrile in contrast to the aqueous solution (PBS or H2O) and possesses environment-sensitive properties with turn-on mechanism[1].
HX103 (5 μM) is non-fluorescent in PBS, but exhibits high fluorescence upon the addition of wild-type or mutant EGFR (L858R and 19del). HX103 is selective toward EGFR wild-type and primary mutants (L858R and 19del), but less sensitive to the acquired resistance mutation EGFR T790M[1].
HX103 has a slightly stronger binding affinity to EGFR L858R (Kd = 0.8 ± 0.3 µM) and EGFR 19del (Kd = 1.1 ± 0.2 µM), when compared with EGFR wild-type (Kd = 2.7 ± 0.4 µM) and the acquired resistance mutation T790M (Kd = 6.6 ± 4.6 µM)[1].
HX103 (0.3-10 μM; 2 h) targets the active site of EGFR-tyrosine kinase and inhibits EGFR activation by competing with ATP[1].

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

HX103 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCC827
Concentration: 0.3, 1, 3 and 10 µM
Incubation Time: 2 h
Result: Inhibited the phosphorylation of EGFR and the downstream proteins (without obviously affecting their total proteins’ levels) in HCC827 cells (EGFR 19del).
Molecular Weight

602.04

Formula

C26H25ClFN7O5S
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

COC1=C(C=C2N=CN=C(C2=C1)NC3=CC(Cl)=C(C=C3)F)OCCCNC4=CC=C(C5=NON=C45)S(=O)(N(C)C)=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 : 50 mg/mL (83.05 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 1.6610 mL 8.3051 mL 16.6102 mL
5 mM 0.3322 mL 1.6610 mL 3.3220 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.

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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 1.6610 mL 8.3051 mL 16.6102 mL 41.5255 mL
5 mM 0.3322 mL 1.6610 mL 3.3220 mL 8.3051 mL
10 mM 0.1661 mL 0.8305 mL 1.6610 mL 4.1525 mL
15 mM 0.1107 mL 0.5537 mL 1.1073 mL 2.7684 mL
20 mM 0.0831 mL 0.4153 mL 0.8305 mL 2.0763 mL
25 mM 0.0664 mL 0.3322 mL 0.6644 mL 1.6610 mL
30 mM 0.0554 mL 0.2768 mL 0.5537 mL 1.3842 mL
40 mM 0.0415 mL 0.2076 mL 0.4153 mL 1.0381 mL
50 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8305 mL
60 mM 0.0277 mL 0.1384 mL 0.2768 mL 0.6921 mL
80 mM 0.0208 mL 0.1038 mL 0.2076 mL 0.5191 mL
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HX103 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:

HX1032566466-98-4HX 103HX-103EGFREpidermal growth factor receptorErbB-1HER1NSCLCEGFR-TKIHCC827Inhibitorinhibitorinhibit

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