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^[1].

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 (K_d = 0.8 ± 0.3 µM) and EGFR 19del (K_d = 1.1 ± 0.2 µM), when compared with EGFR wild-type (K_d = 2.7 ± 0.4 µM) and the acquired resistance mutation T790M (K_d = 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.

602.04

C₂₆H₂₅ClFN₇O₅S

2566466-98-4

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

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• [1]. Deng H, et al. A fluorogenic probe for predicting treatment response in non-small cell lung cancer with EGFR-activating mutations. Nat Commun. 2022 Nov 14;13(1):6944.  [Content Brief]