PD 173955

酪氨酸激酶抑制剂；抑制c-Src、Yes和LCK（IC50s分别为25、22和5nM）以及Bcr-Abl和c-Kit（IC50s分别为1-2和25nM），并且对这些激酶的选择性优于InsR、α-FGFR、bFGFR、PDGFR和PKC；在5,000nM时诱导DU145前列腺、SKOV3卵巢、HT-29结肠、A549肺癌和A431皮肤癌细胞于G2/M期细胞周期停滞；抑制MDA-MB-468和MCF-7乳腺癌细胞（IC50分别为500和1,000nM）以及患者来源的外周血CML祖细胞（IC50=~7.5nM）的增殖。A tyrosine kinase inhibitor; inhibits c-Src, Yes, and LCK (IC50s = 25, 22, and 5 nM, respectively), as well as Bcr-Abl and c-Kit (IC50s = 1-2 and 25 nM, respectively), and is selective for these kinases over InsR, α-FGFR, bFGFR, PDGFR, and PKC; induces cell cycle arrest at the G2/M phase in DU145 prostate, SKOV3 ovarian, HT-29 colon, A549 lung, and A431 skin cancer cell at 5,000 nM; inhibits proliferation of MDA-MB-468 and MCF-7 breast cancer cells (IC50s = 500 and 1,000 nM, respectively), as well as patient-derived peripheral blood CML progenitor cells (IC50= ~7.5 nM).分子式C21H16Cl2N4OS分子量443.4CSC1=CC=CC(NC2=NC=C(C=C(C3=C(Cl)C=CC=C3Cl)C(N4C)=O)C4=N2)=C1