2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. PROTAC BET Degrader-17

PROTAC BET Degrader-17 是一种高效的 BET 蛋白 PROTAC 降解剂。PROTAC BET Degrader-17 通过募集 VHL E3 连接酶，特异性降解 BRD2、BRD3 (DC50=0.09 nM) 和 BRD4 (IC50=4.3 nM)。PROTAC BET Degrader-17 在急性髓系白血病 (AML) 研究中展现出强效抗肿瘤活性，不仅能抑制癌细胞增殖、诱导细胞周期阻滞与凋亡 (apoptosis)，还在异种移植小鼠模型中有效抑制了肿瘤生长。PROTAC BET Degrader-17 可用于探索急性髓系白血病靶向疗法。

(粉色: BET 配体 (HY-169980)；蓝色: VHL 配体 (HY-125845)；黑色: 连接子 (HY-108369))。

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PROTAC BET Degrader-17

PROTAC BET Degrader-17 Chemical Structure

CAS No. : 2409674-38-8

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PROTAC BET Degrader-17 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia[1].
(Pink: BET ligand (HY-169980); Blue: VHL ligand (HY-125845); Black: linker (HY-108369)).

IC50 & Target

VHL

 

BRD4

4.3 nM (IC50)

BRD3

0.09 nM (DC50)

BRD2

 

体外研究
(In Vitro)

PROTAC BET Degrader-17 (Compound A12) 抑制 MV4-11、RAMOS、K562 和 Jurkat 细胞增殖，IC50 (72 h) 分别为 0.570 nM、15.78 nM、57.23 nM、0.621 nM[1]。
PROTAC BET Degrader-17 (0.1-300 nM; 15 min-24 h) 可在 MV4-11 细胞中以时间和剂量依赖的方式诱导 BRD2、BRD3、BRD4 降解，并下调 c-Myc[1]。
PROTAC BET Degrader-17 (0.3-30 nM; 48 h) 可在 MV4-11 细胞中诱导剂量依赖性的 G1 期细胞周期阻滞[1]。
PROTAC BET Degrader-17 (0.3-100 nM; 48 h) 可在 MV4-11 细胞中诱导剂量依赖性凋亡，在 10 nM 以下浓度时其效力优于 ABBV-075 (HY-100015)[1]。
PROTAC BET Degrader-17 在小鼠肝微粒体中具有优异的代谢稳定性，半衰期为 43.88 min，内在清除率为 31.59 mL/min/kg[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC BET Degrader-17 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.3-30 nM
Incubation Time: 48 h
Result: Induced dose-dependent G1 phase cell cycle arrest; as the concentration of PROTAC BET Degrader-17 increased, the percentage of cells in G1 phase increased.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.3-100 nM
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis; at lower concentrations (<10 nM), PROTAC BET Degrader-17 was more potent at inducing apoptosis than ABBV-075, though it did not achieve the maximal apoptotic induction level of A10.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-∞ Cmax T1/2 CL MRT
Mice[1] 1 mg/kg i.v. 1016 ng·h/mL 12403 ng/mL 0.317 h 17.0 mL/min/kg 0.0947 h
Mice[1] 2 mg/kg i.p. 1054 ng·h/mL 581 ng/mL 2.04 h / 2.50 h
体内研究
(In Vivo)

PROTAC BET Degrader-17 (Compound A12) (2 mg/kg；腹腔注射；每两天一次；共 21 天) 可在 MV4-11 AML 异种移植模型中实现 60.5% 的肿瘤生长抑制率，且未出现显著的体重下降[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c nude mice (4 to 5 weeks old)[1]
Dosage: 2 mg/kg
Administration: i.p.; every other day; 21 days
Result: Achieved 60.5% tumor growth inhibition (TGI) relative to vehicle control.
Downregulated BRD4 and c-Myc protein expression in tumor tissue compared to vehicle control.
Caused no significant body weight loss during the study.
分子量

1098.20

Formula

C52H57F2N11O10S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC BET Degrader-17 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC BET Degrader-172409674-38-8PROTAC BET Degrader17PROTAC BET Degrader 17PROTACsEpigenetic Reader DomainApoptosisubiquitin-proteasome systemBRD2acute myeloid leukemia cellsBRD3MV4-11 cellsVHL E3 ligaseBRD4acute myeloid leukemia xenograft mouse modelsJurkat cellsRAMOS cellsInhibitorinhibitorinhibit

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