Degrasyn, also known as WP1130, is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. WP1130 was more effective in reducing leukemic versus normal hematopoietic colony formation and strongly inhibited colony formation of cells derived from patients with T315I mutant Bcr/Abl-expressing CML in blast crisis. WP1130 suppressed the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. WP1130 may be useful in treating CML.
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名称 | WP-1130 |
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Iupac 化学名称 | (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide |
同义词 | WP1130; WP-1130; WP 1130. Degrasyn |
英文同义词 | WP1130; WP-1130; WP 1130. Degrasyn |
分子式 | C19H18BrN3O |
分子量 | 384.27 |
Smile | O=C(N[C@H](C1=CC=CC=C1)CCC)/C(C#N)=C/C2=NC(Br)=CC=C2 |
InChiKey | LIDOPKHSVQTSJY-VMEIHUARSA-N |
InChi | InChI=1S/C19H18BrN3O/c1-2-7-17(14-8-4-3-5-9-14)23-19(24)15(13-21)12-16-10-6-11-18(20)22-16/h3-6,8-12,17H,2,7H2,1H3,(H,23,24)/b15-12+/t17-/m0/s1 |
Cas号 | 856243-80-6 |
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