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

Larotinib 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 Chemical Structure

Larotinib Chemical Structure

CAS No. : 1438072-11-7

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5 mg USD 220 In-stock
10 mg USD 330 In-stock
25 mg USD 560 In-stock
50 mg USD 800 In-stock
100 mg USD 1120 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Larotinib:

Larotinib 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 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)

IRAK1

167 nM (IC50)

BTK

196 nM (IC50)

HER2

253 nM (IC50)

In Vivo

After daily administration of Larotinib mesylate, 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 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

488.94

Formula

C24H26ClFN4O4
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
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 : 125 mg/mL (255.66 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 2.0452 mL 10.2262 mL 20.4524 mL
5 mM 0.4090 mL 2.0452 mL 4.0905 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. 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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V2

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

Dosage

mg/kg

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g

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(per animal)

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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. 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 2.0452 mL 10.2262 mL 20.4524 mL 51.1310 mL
5 mM 0.4090 mL 2.0452 mL 4.0905 mL 10.2262 mL
10 mM 0.2045 mL 1.0226 mL 2.0452 mL 5.1131 mL
15 mM 0.1363 mL 0.6817 mL 1.3635 mL 3.4087 mL
20 mM 0.1023 mL 0.5113 mL 1.0226 mL 2.5566 mL
25 mM 0.0818 mL 0.4090 mL 0.8181 mL 2.0452 mL
30 mM 0.0682 mL 0.3409 mL 0.6817 mL 1.7044 mL
40 mM 0.0511 mL 0.2557 mL 0.5113 mL 1.2783 mL
50 mM 0.0409 mL 0.2045 mL 0.4090 mL 1.0226 mL
60 mM 0.0341 mL 0.1704 mL 0.3409 mL 0.8522 mL
80 mM 0.0256 mL 0.1278 mL 0.2557 mL 0.6391 mL
100 mM 0.0205 mL 0.1023 mL 0.2045 mL 0.5113 mL
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Larotinib 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:

Larotinib1438072-11-7EGFRIRAKBtkEpidermal growth factor receptorErbB-1HER1Interleukin-1 receptor associated kinaseIL-1R associated kinaseBruton tyrosine kinaseadvanced solid tumorHER2HER4BTKBLKtumorInhibitorinhibitorinhibit

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