Imatinib mesylate

Imatinib Mesylate is a cornerstone pharmaceutical intermediate and certified reference standard extensively utilized in the synthesis and quality control of the blockbuster anticancer drug marketed as Gleevec®/Glivec®. As the first approved tyrosine kinase inhibitor, Imatinib Mesylate is indicated for the treatment of chronic myeloid leukemia, Philadelphia chromosome-positive acute lymphoblastic leukemia, myelodysplastic/myeloproliferative diseases, and gastrointestinal stromal tumors driven by activating c-kit mutations. In pharmaceutical quality control contexts, Imatinib Mesylate serves as the primary reference standard for impurity profiling, analytical method development, and regulatory submissions. Imatinib Mesylate is also recognized as an official pharmacopeial reference standard by the European Pharmacopoeia (EP), making it indispensable for ANDA filings and quality control testing for generic imatinib manufacturers. The drug substance Imatinib Mesylate exhibits excellent stability when stored under recommended conditions, with a shelf life of one year from date of purchase as supplied. Furthermore, Imatinib Mesylate functions as a multi-target inhibitor of v-Abl, c-Kit, and PDGFR kinases, demonstrating the broad therapeutic potential of this well-characterized molecular scaffold.

 

Product Parameters

---

Parameter	Specification
Product Name	Imatinib Mesylate
CAS Number	220127-57-1
Molecular Formula	C₃₀H₃₅N₇O₄S
Molecular Weight	589.71 g/mol
Appearance	White to off-white to beige powder
Melting Point	214–224°C
Storage Condition	2–8°C for short-term; –20°C for long-term

Mechanism Of Action

---

Imatinib mesylate inhibits the Bcr-Abl tyrosine kinase at the cellular level both in vitro and in vivo, selectively suppressing proliferation and inducing apoptosis in Bcr-Abl-positive cell lines, Ph-chromosome-positive chronic myeloid leukemia cells, and fresh peripheral blood cells from patients with acute lymphoblastic leukemia. Additionally, imatinib mesylate inhibits the tyrosine kinases of platelet-derived growth factor (PDGF) receptor, stem cell factor (SCF), and c-Kit receptor, thereby blocking PDGF-and SCF-mediated cellular responses. Some patients may develop resistance through various mechanisms.

Bioactivity

---

Imatinib Mesylate (STI571, CGP-57148B) is a bioactive oral imatinib mesylate salt and a multi-target inhibitor that acts on v-AbChemicalbookl, c-Kit, and PDGFR, with IC50 values of 0.6 μM, 0.1 μM, and 0.1 μM respectively in both cell-free and cellular assays. Imatinib Mesylate (STI571) can induce autophagy.

 

In Vitro Study

---

In vitro assays demonstrating inhibition of tyrosine and serine/threonine protein kinases revealed that Imatinib effectively inhibits V-Abl tyrosine kinase and PDGFR with IC50 values of 0.6 μM and 0.1 μM, respectively. Imatinib also suppresses SLF-dependent activation of wild-type c-kit kinase activity at an IC50 of approximately 0.1 μM, a concentration comparable to that required for inhibiting PDGFR. Chemicalbook data indicate that Imatinib exhibits inhibitory effects on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1, with IC50 values of 32.4 μM and 32.8 μM, respectively. Recent studies have demonstrated that Imatinib exerts its antileukemic effect in chronic myeloid leukemia by downregulating the hERG1K(+) channel, which is highly expressed in leukemic cells and promotes leukemia progression.

Contact Us

---

Partner with Cosperpharm for Imatinib Mesylate that meets the highest standards of purity, documentation, and supply reliability. Whether you are advancing a generic imatinib program, developing analytical methods, or scaling up commercial production, our team is ready to support your success.