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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > ABBV-744CAS：2138861-99-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to yellow Solid
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| CAS | 2138861-99-9 |
| Name | ABBV-744 |
| Molecular Formula | C28H30FN3O4 |
| Molecular Weight | 491.55 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Off-white to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD31657409 |
| SMILES | CC(O)(C)C1=CC(C(C2=C3NC(C(NCC)=O)=C2)=CN(C)C3=O)=C(OC4=C(C)C=C(F)C=C4C)C=C1 |
| Target Point | Epigenetic Reader Domain;BRD2、BRD3、BRD4 |
| Passage | Epigenetics |
| Background | ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4. |
| Biological Activity | ABBV-744是一种具有选择性的BET bromodomain强效抑制剂，对 BRD2/3/4 的 BDII 具有特异性，可抑制BRD2、BRD3和BRD4。它可进一步研究用于治疗急性髓细胞性白血病和癌症。ABBV-744 是一种有效且选择性的 AR 转录途径抑制剂。[1] |
| In Vitro | ABBV-744是有效的BDII抑制剂，可抑制BRD2/3/4。对BDII的结合偏好是对BDI的250倍以上，具有良好的药物类属性。RNA-Seq 和 qPCR 显示 ABBV-744 是一种有效且选择性的 AR 转录途径抑制剂。 ChIP-Seq 和 ChIP-qPCR 揭示了 BRD4 从 AR 占据的增强子和启动子中的 BDII 抑制剂置换，这与 AR 对维持致癌基因表达程序的 BRD4 BDII 特异性依赖性一致。[1]。 |
| In Vivo | 在AML和前列腺癌移植瘤模型中，最大耐受剂量的ABBV-744可诱导肿瘤生长抑制作用[1]。 |
| Data Literature Source | [1] Emily J. Faivre，et al. First-in-class，highly BDII-selective BET family inhibitor ABBV-744 displays potent anti-tumor activity in androgen receptor positive prostate cancer models and an improved tolerability profile. Cancer Res. 2018，78(13 Suppl):Abstract nr 4960. |
| Unit | Bottle |
| Specification | 2mg 5mg |
ABBV-744是一种对BDII具有选择性的BET bromodomain抑制剂，可抑制BRD2、BRD3和BRD4。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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