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

Theliatinib  (Synonyms: Xiliertinib; HMPL-309)

Cat. No.: HY-104066 Purity: 99.77%
COA Handling Instructions

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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 (Xiliertinib) 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. Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 264 In-stock
Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Solid
1 mg USD 114 In-stock
5 mg USD 240 In-stock
10 mg USD 390 In-stock
25 mg USD 780 In-stock
50 mg USD 1300 In-stock
100 mg USD 2200 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Theliatinib:

Theliatinib Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Theliatinib (Xiliertinib) 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[1]. Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

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].

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

Theliatinib Related Antibodies
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].

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

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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C[C@]2([H])N(C)CC[C@]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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (11.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMSO : 1 mg/mL (2.26 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; 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 2.2598 mL 11.2992 mL 22.5984 mL
5 mM 0.4520 mL 2.2598 mL 4.5197 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.77%

COA (251 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / DMSO 1 mM 2.2598 mL 11.2992 mL 22.5984 mL 56.4959 mL
DMSO 5 mM 0.4520 mL 2.2598 mL 4.5197 mL 11.2992 mL
10 mM 0.2260 mL 1.1299 mL 2.2598 mL 5.6496 mL
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Theliatinib 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:

Theliatinib1353644-70-8Xiliertinib HMPL-309HMPL309HMPL 309HMPL-309EGFREpidermal growth factor receptorErbB-1HER1ATP-competitiveAKTERKanti-tumoresophagealcancerphosphorylationorallyInhibitorinhibitorinhibit

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