Mobocertinib succinate Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO : 25 mg/mL (35.52 mM; Need ultrasonic)

InChI

InChI=1S/C32H39N7O4.C4H6O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26;5-3(6)1-2-4(7)8/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36);1-2H2,(H,5,6)(H,7,8)

InChIKey

YXYAEUMTJQGKHS-UHFFFAOYSA-N

SMILES

C(C(=O)O)CC(=O)O.C(C1=CN=C(NC2C=C(NC(=O)C=C)C(N(C)CCN(C)C)=CC=2OC)N=C1C1=CN(C)C2=CC=CC=C12)(=O)OC(C)C

Mobocertinib succinate Usage And Synthesis

Description

Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.

Uses

Mobocertinib is an oral targeted therapy drug^[1].Mobocertinib is used to treat a certain type of non-small cell lung cancer (NSCLC) that cannot be removed by surgery and has spread to other parts of the body either during or after treatment with platinum chemotherapy medications.

Mechanism of action

Mobocertinib acts to inhibit EGFR exon 20 insertion mutations at a lower concentration than it does on wild-type proteins.

Side effects

Diarrhoea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin,musculoskeletal pain, increased amylase/lipase/creatinine, and decreased potassium/hemoglobin/magnesium/lymphocytes.

Synthesis

Mobocertinib succinate is prepared by the reaction of Isopropyl 2-chloro-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate in the presence of an inert atmosphere.

References

[1] IMRANMOHD. Discovery, Development, Inventions, and Patent Trends on Mobocertinib Succinate: The First-in-Class Oral Treatment for NSCLC with EGFR Exon 20 Insertions.[J]. Biomedicines, 2021. DOI:10.3390/biomedicines9121938.