2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  3. PROTACs FLT3 JAK Epigenetic Reader Domain
  4. PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 是一种 PROTAC 降解剂，针对 FLT3、JAK2 和 BRD4，DC50 值分别为 5.23 nM、0.678 nM 和 1.17 nM。PROTAC FLT3/JAK2/BRD4 Degrader-1 对 MV4;11 细胞 (IC50 = 0.79 nM) 和 FLT3 突变转化的 Ba/F3 细胞表现出强效的抗增殖活性。PROTAC FLT3/JAK2/BRD4 Degrader-1 诱导 MV4;11 细胞凋亡 (apoptosis)。PROTAC FLT3/JAK2/BRD4 Degrader-1 在 NOD SCID 小鼠建立的 MV4;11 异种移植模型中展示出显著的抗肿瘤效能。PROTAC FLT3/JAK2/BRD4 Degrader-1 可用于急性髓系白血病 (AML) 的研究。(粉色：FLT3/JAK2/BRD4 配体：(HY-175611)，蓝色：CRBN 配体 (HY-W087383)，黑色：连接子，E3 连接酶配体-连接子偶联物：(HY-W897939))。

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PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 Chemical Structure

CAS No. : 3067695-20-6

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PROTAC FLT3/JAK2/BRD4 Degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 JAK 亚型特异性产品:

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939))[1].

IC50 & Target[1]

Cereblon

 

BRD4

1.17 nM (DC50)

JAK2

0.678 nM (DC50)

FLT3

5.23 nM (DC50)

体外研究
(In Vitro)

PROTAC FLT3/JAK2/BRD4 Degrader-1 (Compound 13e) 在 MV4;11 细胞中降解 FLT3、JAK2 和 BRD4，其 DC50 值分别为 5.23 nM、0.678 nM 和 1.17 nM[1]。
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1 μM, 8 h) 在 MV4;11 细胞中通过泛素-蛋白酶体系统 (UPS) 诱导依赖于 cereblon 和蛋白酶体的 FLT3、JAK2 和 BRD4 降解[1]。
PROTAC FLT3/JAK2/BRD4 Degrader-1 (0.00001-1000 nM, 96 h) 强效抑制 MV4;11 细胞增殖，IC50 为 0.79 nM[1]。
PROTAC FLT3/JAK2/BRD4 Degrader-1 (96 h) 对 FLT3 突变转化的 Ba/F3 细胞表现出强效的抗增殖活性，包括 FLT3-ITD-D835Y (IC50 = 35.64 nM)、FLT3-ITD-F691L (IC50 = 24.34 nM)、FLT3-ITD-N676D (IC50 = 43.71 nM)、FLT3-ITD-D835V (IC50 = 6.63 nM)、FLT3-ITD-Y842C (IC50 = 8.80 nM) 和 FLT3-ITD (IC50 = 28.62 nM)[1]。
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1-1000 nM, 48 h) 在 MV4;11 细胞中诱导超过 70% 的细胞凋亡[1]。

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

PROTAC FLT3/JAK2/BRD4 Degrader-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: MV4;11 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 48 h
Result: Induced over 70% apoptosis in MV4;11 cells.
Suppressed activated apoptotic proteins PARP, Caspase 9, Caspase 3.
Upregulated Cleaved-caspase 3.
体内研究
(In Vivo)

PROTAC FLT3/JAK2/BRD4 Degrader-1 (Compound 13e) (10 mg/kg，腹腔给药，每日一次，持续 21 天) 在 NOD SCID 小鼠建立的 MV4;11 异种移植模型中展示出显著的抗肿瘤效能[1]。

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

Animal Model: MV4;11 cells (3 × 106) were subcutaneously implanted into the right flanks of four-week-old female nonobese diabetic severe combined immune-deficiency (NOD SCID) mice to establish the MV4;11 xenograft model[1]
Dosage: 10 mg/kg
Administration: i.p., once daily, 21 days
Result: Achieved a tumor growth inhibition (TGI) rate of 62% at a dose of 10 mg/kg in the MV4;11 xenograft model.
Showed no significant changes in body weight.
分子量

883.00

Formula

C44H51FN10O7S
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 FLT3/JAK2/BRD4 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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 FLT3/JAK2/BRD4 Degrader-13067695-20-6PROTACsFLT3JAKEpigenetic Reader DomainCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Janus kinaseacute myeloid leukemia (AML)PROTACJAK2BRD4MV4;11 cellsInhibitorinhibitorinhibit

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