E-7449
E-7449 Basic information
- Product Name:
- E-7449
- Synonyms:
-
- E7449
- 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
- CAS:
- 1140964-99-3
- MF:
- C18H15N5O
- MW:
- 317.34
- 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-7449Supplier
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- +86-19182167371 +86-19182167371;
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- 021-58950125
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- +86-21-5821 5861
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