2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Immunology/Inflammation
  3. EGFR IRAK Btk
  4. Larotinib mesylate hydrate

Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.

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

Larotinib mesylate hydrate Chemical Structure

Larotinib mesylate hydrate Chemical Structure

CAS No. : 2097129-93-4

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5 mg USD 245 In-stock
10 mg USD 380 In-stock
25 mg USD 800 In-stock
50 mg USD 1280 In-stock
100 mg USD 2100 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Larotinib mesylate hydrate:

Larotinib mesylate hydrate Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All IRAK Isoform Specific Products:

View All Isoforms
IRAK1 IRAK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM[1].

IC50 & Target[1]

EGFRL861Q

0.423 nM (IC50)

EGFRL858R

0.563 nM (IC50)

EGFR (WT)

0.611 nM (IC50)

EGFRT790M

45.2 nM (IC50)

HER4

84 nM (IC50)

BLK

102 nM (IC50)

IRAK-1

167 nM (IC50)

BTK

196 nM (IC50)

HER2

253 nM (IC50)

In Vivo

After daily administration of Larotinib mesylate hydrate, the no observed adverse effect level (NOAEL) is 10 mg/kg in Sprague-Dawley rats and the lowest observed adverse effect level (LOAEL) is 5 mg/kg in beagle dogs. The maximal tolerable doses (MTDs) are 20 and 25 mg/kg in Sprague-Dawley rats and beagle dogs, respectively[1].
Larotinib mesylate hydrate shows dose-dependent antitumor results and a tumor-inhibiting rate exceeding 60% at 18 mg/kg in a tumor-bearing mice model (data not published)[1].

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

699.17

Formula

C26H36ClFN4O11S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC(C(OCCCN1C[C@]2([H])[C@](OCCO2)([H])C1)=C3)=CC4=C3C(NC5=CC(Cl)=C(C=C5)F)=NC=N4.CS(=O)(O)=O.CS(=O)(O)=O.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (35.76 mM; Need ultrasonic; 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 1.4303 mL 7.1513 mL 14.3027 mL
5 mM 0.2861 mL 1.4303 mL 2.8605 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4303 mL 7.1513 mL 14.3027 mL 35.7567 mL
5 mM 0.2861 mL 1.4303 mL 2.8605 mL 7.1513 mL
10 mM 0.1430 mL 0.7151 mL 1.4303 mL 3.5757 mL
15 mM 0.0954 mL 0.4768 mL 0.9535 mL 2.3838 mL
20 mM 0.0715 mL 0.3576 mL 0.7151 mL 1.7878 mL
25 mM 0.0572 mL 0.2861 mL 0.5721 mL 1.4303 mL
30 mM 0.0477 mL 0.2384 mL 0.4768 mL 1.1919 mL
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Larotinib mesylate hydrate 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:

Larotinib mesylate2097129-93-4EGFRIRAKBtkEpidermal growth factor receptorErbB-1HER1Interleukin-1 receptor associated kinaseIL-1R associated kinaseBruton tyrosine kinaseadvanced solid tumorHER2HER4BTKBLKtumorInhibitorinhibitorinhibit

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