alpha-IMATINIB MESYLATE
Imatinib Mesylate
CAS: 220127-57-1
Molecular Formula: C30H35N7O4S
alpha-IMATINIB MESYLATE - Names and Identifiers
| Name | Imatinib Mesylate |
| Synonyms | Glivec STI-571 gleevec Imatinibmesylate Imatinib Mesylate imatinib mesilate IMATINIB BASE(IMA-3) alpha-IMATINIB MESYLATE imatinib methanesulfonate Imatinib mesylate(TINIBS ) Imatinib mesylate(Alpha form) IMATINIB MESYLATE (IMATINIB METHANESULFONATE) Imatinib Methanesulfonate, STI-571, CGP-57148B, Glivec, 4-[(4-methylpiperazin-1-yl)methyl]-n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate 4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate |
| CAS | 220127-57-1 |
| EINECS | 606-892-3 |
| InChI | InChI=1/C29H31N7O.CH4O3S/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36;1-5(2,3)4/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34);1H3,(H,2,3,4) |
| InChIKey | YLMAHDNUQAMNNX-UHFFFAOYSA-N |
alpha-IMATINIB MESYLATE - Physico-chemical Properties
| Molecular Formula | C30H35N7O4S |
| Molar Mass | 589.71 |
| Melting Point | 214-224°C |
| Boling Point | 133-134 ℃(lit.) |
| Solubility | Soluble in water (200 mg/ml), ethanol (~0.2 mg/ml), DMSO (200 mg/ml), DMF (~10 mg/ml) |
| Appearance | Crystallization |
| Color | white to beige |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 3 months. |
| Physical and Chemical Properties | Properties: pale yellow or white crystalline powder |
| Use | Imatinib intermediates |
| In vitro study | In vitro assays for inhibition of tyrosine and serine/threonine protein kinases showed that Imatinib potently inhibited V-Abl tyrosine kinases and PDGFR with an IC50 of 0.6 μm and 0.1 μm, respectively. Imatinib inhibits SLF-dependently activated wild-type c-kit kinase activity with IC 50 at approximately 0.1 μm, which is similar to the concentration required to inhibit PDGFR. Imatinib exhibited inhibitory effects on human bronchial carcinoid cell line NCI-H727 and human pancreatic carcinoid cell line BON-1 with IC50 of 32.4 μm and 32.8 μm, respectively. A recent study showed that Imatinib exerts an anti-leukemia effect in chronic myeloid leukemia by down-regulating the hERG1 K() channel, which is highly expressed in leukemia cells and appears to be conducive to the emergence of leukemia. |
| In vivo study | Imatinib inhibited SCLC6,SCLC61, and SCLC108 xenograft tumors derived from fresh surgical samples of human small cell lung cancer by 80%,40%, and 78%, respectively, and there was no significant inhibition on the growth of sclc74. In high-fat-fed ApoE(-/-) mice administered 10 mg/kg,20 mg/kg, and 40 mg/kg Imatinib by gavage, compared with the control group, the lipid staining area induced by high fat was reduced by 30%,27% and 35%, and the carotid lipid accumulation was inhibited. |
alpha-IMATINIB MESYLATE - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
| RTECS | CV5520550 |
| HS Code | 29350090 |
alpha-IMATINIB MESYLATE - Introduction
Imatinib Mesylate (STI571) is a Imatinib methanesulfonate with good oral bioavailability and is a multi-target inhibitor. It acts on v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM respectively.
Last Update：2022-10-16 17:15:01
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