N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-hydroxybutanedioate
Sunitinib malate
CAS: 341031-54-7
Molecular Formula: C26H33FN4O7
N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-hydroxybutanedioate - Names and Identifiers
| Name | Sunitinib malate |
| Synonyms | SU112248 SU 011248 Malic acid Shu Sunitinib malate SUNITINIB MALEATE Butanedioic acid, 2 Sunitinib Malate(SU 11248) EZSolution Sunitinib Malate N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1 N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-hydroxybutanedioate |
| CAS | 341031-54-7 |
| EINECS | 638-825-9 |
| InChI | InChI=1/C23H30N4O2.C5H8O5/c1-6-27(7-2)11-10-24-23(29)21-15(4)20(25-16(21)5)13-18-17-12-14(3)8-9-19(17)26-22(18)28;6-3(5(9)10)1-2-4(7)8/h8-9,12-13,25H,6-7,10-11H2,1-5H3,(H,24,29)(H,26,28);3,6H,1-2H2,(H,7,8)(H,9,10)/b18-13-;/t;3-/m.0/s1 |
| InChIKey | XGQXULJHBWKUJY-LYIKAWCPSA-N |
N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-hydroxybutanedioate - Physico-chemical Properties
| Molecular Formula | C26H33FN4O7 |
| Molar Mass | 532.57 |
| Melting Point | 189-191°C |
| Solubility | DMSO: >10mg/mL |
| Appearance | powder |
| Color | Orange |
| Storage Condition | room temp |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | Sunitinib is also a potent c-Kit inhibitor with an IC50 of 211 nM. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ, with K I of 9 nM and 8 nM, respectively, acting on VEGFR2 and PDGFR than on FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src selectivity is more than 10 times higher. Sunitinib acts on serum starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, inhibiting VEGF-dependent phosphorylation of VEGFR2 and PDGFR-dependent phosphorylation of pdgfβ, with an IC50 of 10 nM and 10 nM. Sunitinib inhibited the proliferation of VEGF-induced serum-starved HUVECs with an IC50 of 40 nM, and inhibited PDGF-induced NIH-3T3 cells overexpressing PDGFRβ or PDGFRα, IC50 was 39 nM and 69 nM, respectively. Sunitinib inhibited wild-type FLT3, FLT3-ITD, and FLT3-Asp835 phosphorylation with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits MV4;11 and OC1-AML5 cell proliferation with IC50 of 8 nM and 4 nM, respectively, And induce apoptosis in a dose-dependent manner. |
| In vivo study | Consistent with a large and selective inhibition of VEGFR2 or PDGFR phosphorylation and signal in vivo, Sunitinib treats a variety of transplanted tumor models at a dose of 20-80 mg/kg per day, including HT-29, A431, Colo205, H-460, SF763T, c6, A375, or MDA-MB-435, has broad and potent anticancer activity in a dose-dependent manner. Treatment of Sunitinib at a dose of 80 mg/kg daily for 21 days resulted in complete tumor regression in six of the eight mice, and no tumor recurrence was observed for 110 days after the end of the treatment. A second round of treatment with Sunitinib was still highly effective on tumors that did not completely decline in the first round. Treatment of SF763T glioma with Sunitinib resulted in a significant decrease in tumor MVD by ~ 40%. SU11248 treatment completely inhibited the growth of PC-3M xenografts expressing luciferase, while the tumor size did not decrease. Sunitinib at a dose of 20 mg/kg per day significantly blocked subcutaneous MV4;11 (FLT3-ITD) xenograft growth and inhibited prolonged lifespan in a FLT3-ITD bone marrow xenograft model. |
N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-hydroxybutanedioate - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | R61 - May cause harm to the unborn child R2 - Risk of explosion by shock, friction, fire or other sources of ignition R48/25 - R36/37 - Irritating to eyes and respiratory system. R22 - Harmful if swallowed R53 - May cause long-term adverse effects in the aquatic environment |
| Safety Description | S53 - Avoid exposure - obtain special instructions before use. S22 - Do not breathe dust. S36/37 - Wear suitable protective clothing and gloves. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 2 |
| HS Code | 29337900 |
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Multiple SpecificationsSpot supply
Product Name: Sunitinib Visit Supplier Webpage Request for quotationCAS: 341031-54-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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