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My CartCAS：1628607-64-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 1628607-64-6 |
| Name | INCB-054329 |
| Molecular Formula | C19H16N4O3 |
| Molecular Weight | 348.36 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | O=C1NC2=C3N1[C@@H](C4=NC=CC=C4)COC3=C(C5=C(C)ON=C5C)C=C2 |
| Target Point | BET |
| Passage | Epigenetics |
| Background | INCB-054329 is a BET inhibitor. |
| Biological Activity | INCB054329 (INCB-054329, INCB-54329)是BET抑制剂，对BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1和BRDT-BD2的IC50分别为44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM和63 nM。[1-3] |
| In Vitro | 3 μM的INCB054329对16种非BET溴区没有显著抑制活性。在含有32种从急性髓性白血病、非霍奇金淋巴瘤和多发性骨髓瘤中分离的血液病癌细胞系中，INCB054329的平均GI50为152 nM。而在正常志愿者体内分离的T细胞中，离体以IL2刺激，INCB054329对其GI50值为2.435 μM。其对细胞的生长抑制作用于细胞于G1期阻滞有关。INCB054828还是FGFR1、2、3的选择性抑制剂[1]。INCB054329可减少同源重组组分的表达，减少细胞生长、增强PARPi和cisplatin诱导的DNA损伤和凋亡[3]。 |
| In Vivo | 在小鼠中，INCB054329具有高清除率，短半衰期。在足以有效地抑制c-myc的暴露量下，INCB054329在KMS-12-BM和MM1.S移植瘤模型中有效并耐受良好[1]。在体内，口服INCB054329在多种血液癌症模型中抑制肿瘤生长[2]。 |
| Cell Experiment | Animal Models: KMS-12-BM移植瘤模型(female Nu/Nu mice); Dosages: 3，10，30或100 mg/kg; Administration: 口服[1] |
| Animal Experiment | 在骨髓瘤细胞系中，INCB054329的处理可抑制c-myc的表达、诱导HEXIM1。在AML和淋巴瘤细胞株中，INCB054329诱导细胞凋亡，促凋亡的调节子表达升高[2]。 |
| Data Literature Source | [1] Stubbs MC，et al. Clin Cancer Res. 2019，25(1):300-311. [2] Phillip CC Liu，et al. AACR Cancer Res. 2015，75(15 Suppl):Abstract nr 3523. [3] Wilson AJ，et al. Gynecol Oncol. 2018，149(3):575-584. |
| Unit | Bottle |
| Specification | 2mg 5mg |
INCB-054329是BET抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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