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公司地址
苏州工业园区生物纳米园A4#216
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4000-520-616 / 18915418616
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0512-67156496
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info@ebiomall.com
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https://www.ebiomall.com
商品描述
| Description | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. | ||
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| Targets |
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| In vitro | Cell lines carrying MLL-rearrangements are selectively responsive to VTP50469. VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding leads to changes in gene expression, differentiation, and apoptosis.[2] | ||
| In vivo | Patient-derived xenograft (PDX) models derived from patients with either MLL-r AML or MLL-r ALL shows dramatic reductions of leukemia burden when treated with VTP50469. Multiple mice engrafted with MLL-r ALL remains disease free greater than one year after treatment.[2] |
