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| Product Name: | E-7449 | | Synonyms: | E-7449;8-(1,3-dihydro-isoindol-2-ylmethyl)-2,9-dihydro-1,2,7,9-tetraaza-phenalen-3-one;E7449;E 7449;3H-Pyridazino[3,4,5-de]quinazolin-3-one, 8-[(1,3-dihydro-2H-isoindol-2-yl)methyl]-1,2-dihydro-;UNII-9X5A2QIA7C;Stenoparib (E7449);E7449,PARP,Inhibitor,inhibit,E 7449,E-7449,poly ADP ribose polymerase;Stenoparib, E7449, 2X-121 | | CAS: | 1140964-99-3 | | MF: | C18H15N5O | | MW: | 317.34 | | EINECS: | | | Product Categories: | | | Mol File: | 1140964-99-3.mol |  |
| | E-7449 Chemical Properties |
| density | 1.53±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:0.2(Max Conc. mg/mL);0.63(Max Conc. mM) | | form | A crystalline solid | | pka | 9.51±0.20(Predicted) | | color | Light yellow to yellow | | InChI | InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21) | | InChIKey | JLFSBHQQXIAQEC-UHFFFAOYSA-N | | SMILES | N1=C2C3C(C(=O)NNC=3N=C1CN1CC3=C(C1)C=CC=C3)=CC=C2 |
| | E-7449 Usage And Synthesis |
| Uses | E 7449 is a dual inhibitor of PARP1/2 and tankyrase1/2 exhibits anti-tumor activity in BRCA-deficient in vivo models. PARP1/2 and tankyrase1/2 are involved with DNA damage and canonical Wnt/β-catenin signaling, respectively. | | in vivo | Stenoparib moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model. Stenoparib (30 or 100 mg/kg, p.o.) inhibits PARP, shows anti-tumor activity, and is well-tolerated without any obvious body weight loss or deaths in a BRCA mutant xenograft model. Stenoparib (30, 100 or 300 mg/kg, p.o.) suppresses re-growth of hair in a dose dependent manner, and blocks Wnt signaling in C57BL/6 mice. Stenoparib (100 mg/kg, p.o.) combined with MEK inhibitor exhibits antitumor activity in a Wnt1 subcutaneous model (mammary tumors initially isolated from Wnt1 (int-1) transgenic mice)[1]. | | IC 50 | PARP2: 1 nM (IC50); PARP1: 2 nM (IC50); TNKS1: 50 nM (IC50); TNKS2: 50 nM (IC50) |
| | E-7449 Preparation Products And Raw materials |
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