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| | KGWWHPZQLVVAPT-STTJLUEPSA-N Basic information |
| Product Name: | KGWWHPZQLVVAPT-STTJLUEPSA-N | | Synonyms: | KGWWHPZQLVVAPT-STTJLUEPSA-N;ENMD 2076;ENMD2076;(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine (2R,3R)-2,3-dihydroxysuccinate(1:1);L-(+) Tartrate salt of ENMD-981693;6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-4-pyrimidinamine, 2R,3R-dihydroxybutanedioate;4-Pyrimidinamine, 6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(1E)-2-phenylethenyl]-, (2R,3R)-2,3-dihydroxybutanedioate (1:1) | | CAS: | 1453868-32-0 | | MF: | C21H25N7.C4H6O6 | | MW: | 525.56 | | EINECS: | | | Product Categories: | | | Mol File: | 1453868-32-0.mol |  |
| | KGWWHPZQLVVAPT-STTJLUEPSA-N Chemical Properties |
| solubility | DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml | | form | A crystalline solid | | color | Light brown to khaki |
| | KGWWHPZQLVVAPT-STTJLUEPSA-N Usage And Synthesis |
| Uses | ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. | | in vivo | ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[1]. | | IC 50 | Aurora A: 1.86 nM (IC50); KDR: 58.2 nM (IC50); Flt-4: 15.9 nM (IC50); FGFR1: 92.7 nM (IC50); FGFR2: 70.8 nM (IC50); PDGFRα: 56.4 nM (IC50); Flt3: 14 nM (IC50) | | References | [1] Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37. DOI:10.1158/1535-7163.MCT-10-0574
[2] Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25. DOI:10.1111/j.1365-2141.2010.08248.x |
| | KGWWHPZQLVVAPT-STTJLUEPSA-N Preparation Products And Raw materials |
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