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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Larotinib mesylate hydrate) usually boasts enhanced water solubility and stability.

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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Larotinib Related Antibodies

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

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IRAK1 IRAK4

  • Biological Activity

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  • References

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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Larotinib Related Classifications

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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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