E7449

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP19934CAS No. ：1140964-99-3Purity：98%

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CAS No.	1140964-99-3	Cat. No.	BCP19934
Name	E7449
Synonyms	E-7449;E 7449;
SMILES
Chemical Name
Formula	C18H15N5O	M. Wt	317.34
Purity	98%	Storage	Store at 4-8°C
Description	E7449 is an orally bioavailable, potent, small molecule inhibitor of Poly(ADP-ribose) Polymerase (PARP)1 and PARP2. E7449 potently inhibits PARP1 and PARP2 in a cell-free assay and potentiates the cytotoxicity of both radiotherapy and chemotherapy. The cytotoxic effect of radiotherapy was enhanced by E7449 in clonogenic survival assays. The anti-tumor activity of the alkylating agent temozolomide was potentiated by E7449 in a dose responsive manner in vivo in the B16-F10 melanoma isograft mouse model. Daily dosing of E7449 as a single agent significantly inhibited tumor growth in a genetically engineered BRCA1 null mouse ovarian xenograft model. In the BRCA1 mutant human breast cancer cell line MDA-MB-436, E7449 significantly inhibited proliferation in a long term growth inhibition assay in vitro. Oral administration of E7449 once daily potently inhibited tumor growth in the MDA-MB-436 xenograft model with no toxicity observed. A dose responsive pharmacodynamic effect on PARP activity