2566466-98-4
2566466-98-4 structure
- Name: HX103
- Chemical Name: HX103
- CAS Number: 2566466-98-4
- Molecular Formula: C26H25ClFN7O5S
- Molecular Weight: 602.04
- Catalog: Signaling Pathways JAK/STAT Signaling EGFR
- Create Date: 2023-01-30 17:27:06
- Modify Date: 2024-02-16 19:31:16
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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 drug sensitivity in NSCLC patients with EGFR-activating mutations[1].
| Name | HX103 |
|---|
| 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 drug sensitivity in NSCLC patients with EGFR-activating mutations[1]. |
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| Related Catalog | |
| Target |
EGFRdel19:1.3 nM (IC50) EGFRL858R:1.5 nM (IC50) EGFRWT:4.0 nM (IC50) EGFRT790M:977 nM (IC50) |
| In Vitro | 与 PBS 或 H2O 水溶液相比，HX103 在乙腈中具有显著的荧光增强作用，并具有环境敏感性质[1]。 HX103 (5 μM) 在 PBS 中不发荧光，但在加入野生型或突变型 EGFR (L858R 和 19del) 后显示出高荧光。HX103 对 EGFR 野生型和主要突变体 (L858R和19del) 具有选择性，但对获得性耐药突变 EGFR T790M 较不敏感[1]。 与 EGFR 野生型 (Kd = 2.7 ± 0.4 µM)和获得性耐药突变型 T790M (Kd = 6.6 ± 4.6µM) 相比，HX103 对 EGFR L858R (Kd = 0.8 ± 0.3 µM) 和 EGFR 19del (Kd = 1.1 ± 0.2 µM) 具有稍强的结合亲和力[1]。 HX103 (0.3-10 μM; 2 h) 靶向 EGFR-酪氨酸激酶的活性位点，通过与 ATP 竞争抑制 EGFR的激活[1]。 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). |
| References |
| Molecular Formula | C26H25ClFN7O5S |
|---|---|
| Molecular Weight | 602.04 |