$CHIR-124 Size:10mg solid Smiles: C[C@]1(O)[C@H](O)[C@@H](C)CC=CC=C[C@H](CC[C@H]2O[C@@]3(CC[C@@H](C)[C@@H](/C=C(/C)\O)O3)[C@H](C)[C@@H](OC(=O)C=C[C@@H](C)[C@H](O)[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C1=O)[C@H]2C)CC |t:8$

CHIR-124 Size:10mg solid Smiles: C[C@]1(O)[C@H](O)[C@@H](C)CC=CC=C[C@H](CC[C@H]2O[C@@]3(CC[C@@H](C)[C@@H](/C=C(/C)\O)O3)[C@H](C)[C@@H](OC(=O)C=C[C@@H](C)[C@H](O)[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C1=O)[C@H]2C)CC |t:8

Name: CHIR-124 Size:10mg solid Smiles: C[C@]1(O)[C@H](O)[C@@H](C)CC=CC=C[C@H](CC[C@H]2O[C@@]3(CC[C@@H](C)[C@@H](/C=C(/C)\O)O3)[C@H](C)[C@@H](OC(=O)C=C[C@@H](C)[C@H](O)[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C1=O)[C@H]2C)CC |t:8
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Description

Smiles: C[C@]1(O)[C@H](O)[C@@H](C)CC=CC=C[C@H](CC[C@H]2O[C@@]3(CC[C@@H](C)[C@@H](/C=C(/C)\O)O3)[C@H](C)[C@@H](OC(=O)C=C[C@@H](C)[C@H](O)[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C1=O)[C@H]2C)CC |t:8

preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells

37 and 97% TGI

AEE788 has significantly smaller tumors and complete inhibition of lymph node metastasis

CHIR-124 Size:10mg solid Smiles: C[C@]1(O)[C@H](O)[C@@H](C)CC=CC=C[C@H](CC[C@H]2O[C@@]3(CC[C@@H](C)[C@@H](/C=C(/C)\O)O3)[C@H](C)[C@@H](OC(=O)C=C[C@@H](C)[C@H](O)[C@@H](C)C(=O)[C@@H](C)[C@H](O)[C@@H](C)C1=O)[C@H]2C)CC |t:8CHIR 124 is a quinolone based small molecule Chk1 inhibitor, that is structurally unrelated to other known inhibitors of Chk1. It potently and selectively inhibits Chk1 in vitro (IC(50) = 0. 0003 micromol L). CHIR 124 interacts synergistically with topoisomerase poisons (e. g., camptothecin or SN 38) in causing growth inhibition in several p53 mutant solid tumor cell lines as determined by isobologram or response surface analysis. CHIR 124 is a novel

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