1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Theliatinib

Theliatinib (Synonyms: HMPL-309)

Cat. No.: HY-104066 Purity: 99.88%
Handling Instructions

Theliatinib (HMPL-309) est un inhibiteur de EGFR qui est puissant, ATP-compétitif, oralement actif et hautement sélectif avec un Ki de 0,05 nM un IC50 de 3 nM. Theliatinib a un IC50 de 22 nM pour le EGFR T790M/L858R mutant. Théliatinib montre une sélectivité> de 50 fois pour EGFR que pour les autres kinases. Activité antitumorale.

Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.

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

Theliatinib Chemical Structure

Theliatinib Chemical Structure

CAS No. : 1353644-70-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 234 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 390 In-stock
Estimated Time of Arrival: December 31
25 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
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Description

Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity[1].

IC50 & Target

EGFR

3 nM (IC50)

EGFR

0.05 nM (Ki)

EGFR (L858R/T790M)

22 nM (IC50)

In Vitro

Theliatinib significantly inhibits EGFR phosphorylation in A431 cells with an IC50 of 7 nM. Theliatinib also inhibits A431, H292 and FaDu cells survival with IC50 values of 80 nM, 58 nM and 354 nM, respectively[1].

In Vivo

Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response[1].

Animal Model: NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)[1]
Dosage: 2 mg/kg, 5 mg/kg, 15 mg/kg
Administration: Oral administration;daily; for 21 days
Result: Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.
Clinical Trial
Molecular Weight

442.51

Formula

C₂₅H₂₆N₆O₂

CAS No.

1353644-70-8

SMILES

O=C(N1C[[email protected]]2([H])N(C)CC[[email protected]]2([H])C1)NC3=CC4=C(NC5=CC=CC(C#C)=C5)N=CN=C4C=C3OC

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 : 5 mg/mL (11.30 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2598 mL 11.2992 mL 22.5984 mL
5 mM 0.4520 mL 2.2598 mL 4.5197 mL
10 mM 0.2260 mL 1.1299 mL 2.2598 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

TheliatinibHMPL-309HMPL309HMPL 309EGFREpidermal growth factor receptorErbB-1HER1ATP-competitiveAKTERKanti-tumoresophagealcancerphosphorylationorallyInhibitorinhibitorinhibit

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Theliatinib
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