Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 60.00 | |
5 mg | In stock | $ 182.00 | |
10 mg | In stock | $ 298.00 | |
25 mg | In stock | $ 491.00 | |
50 mg | In stock | $ 729.00 | |
100 mg | In stock | $ 987.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 191.00 |
Description | Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively. |
Targets&IC50 | EGFR:0.05 nM (Ki), EGFR:3 nM (IC50), EGFR (L858R/T790M):22 nM (IC50) |
In vitro | In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity. |
In vivo | In vivo data demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431, Bcap-37 and Fadu. Two PDECX models with EGFR gene amplification (PDECX1T0326 and PDECX1T0950) were sensitive to theliatinib treatment demonstrating tumor regression of 32% and 75%, respectively. |
Animal Research | Seven- to nine week old NOD-SCID immunodeficient or BALB/cASlac-nu/nu male or female mice. Fresh tumor specimens from newly diagnosed patients were collected during surgery and separated into three parts for the following: (1) To prepare formalin fixed paraffin embedded (FFPE) sections; (2) For snap freezing in liquid nitrogen for DNA extraction and sequencing and (3) For subcutaneous implantation into NOD-SCID mice (P0) and subsequent passages in additional NOD-SCID or nude mice once the tumor size reached 800~1500 mm^3. After several consecutive in vivo passages, the PDECX models (P3~P7) were used to evaluate the anti-tumor efficacy of theliatinib or gefitinib or AZD4547. |
Molecular Weight | 442.51 |
Formula | C25H26N6O2 |
CAS No. | 1353644-70-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 47 mg/mL (106.21 mM)
You can also refer to dose conversion for different animals. More
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Theliatinib 1353644-70-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR ATP-competitive inhibit ERK cancer esophageal Epidermal growth factor receptor HMPL-309 anti-tumor Inhibitor ErbB-1 HMPL309 HER1 HMPL 309 orally Xiliertinib AKT phosphorylation inhibitor