2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs FAK
  4. BSJ-04-146

BSJ-04-146 是一种高效且选择性的 PROTAC 靶向黏着斑激酶 (FAK) 抑制剂 (IC50 = 26 nM)。BSJ-04-146 可在癌细胞中快速有效地降解 FAK，且具有高度的蛋白质组特异性，并在小鼠体内诱导持久降解。BSJ-04-146 与 FAK 结合，并需要泛素-蛋白酶体系统才能实现 FAK 的降解。BSJ-04-146 可用于胰腺癌和三阴性乳腺癌的研究。
(粉色: FAK 配体 (HY-151010)；蓝色: Cereblon 配体 (HY-103597)；黑色: 连接子)。

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BSJ-04-146

BSJ-04-146 Chemical Structure

CAS No. : 2414478-45-6

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BSJ-04-146 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

BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC50 = 26 nM). BSJ-04-146 achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 can be used for the study of pancreatic cancer and triple-negative breast cancer[1]. (Pink: FAK ligand (HY-151010); Blue: Cereblon ligand (HY-103597); Black: linker).

体外研究
(In Vitro)

BSJ-04-146 (1-1000 nM，4 h) 可有效降解 PATU-8988T 细胞中的 FAK 蛋白[1]。
BSJ-04-146 (100 nM，1-24 h) 可快速诱导 PATU-8988T 细胞中 FAK 降解，并同时显著降低 pAKT 信号传导[1]。
BSJ-04-146 (120 h) 显著抑制 PATU-8988T 和 MDA-MB-231 细胞的 3D 球体活力[1]。
BSJ-04-146 (100 nM，4-24 h) 可显著改变 PATU-8988T 细胞中 74 pY 和 161 pY-IMAC 磷酸肽的表达 (包括 FAK 自磷酸化位点的下调)；该改变在处理 24 小时后仍然存在[1]。

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

BSJ-04-146 相关抗体:

Western Blot Analysis[1]

Cell Line: PATU-8988T cells
Concentration: 100 nM
Incubation Time: 1 h, 2 h, 4 h, 8 h, 24 h
Result: Induced FAK degradation in PATU-8988T cells and simultaneously significantly reduced pAKT signaling.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice 10 mg/kg i.p. T1/2 6.1 h
Mice 2 mg/kg i.v. T1/2 3.5 h
Mice 10 mg/kg i.p. Tmax 1 h
Mice 2 mg/kg i.v. Tmax 0.5 h
Mice 10 mg/kg i.p. Cmax 747 ng/mL
Mice 2 mg/kg i.v. Cmax 5897 ng/mL
Mice 10 mg/kg i.p. AUClast 222533 min·ng/mL
Mice 2 mg/kg i.v. AUClast 287736 min·ng/mL
Mice 10 mg/kg i.p. AUCINF_obs 406707 min·ng/mL
Mice 2 mg/kg i.v. AUCINF_obs 304143 min·ng/mL
Mice 2 mg/kg i.v. Vss_obs 0.68 L/kg
体内研究
(In Vivo)

BSJ-04-146 (15-50 mg/kg，腹腔注射，每两天一次 (三次) 或单次给药) 可诱导 PATU-8988T 细胞异种移植小鼠中持久且全身性的 FAK 降解，且小鼠耐受性良好[1]。

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

Animal Model: Two million PATU-8988T cells were suspended in PBS and subcutaneously injected into the right groin of nude female mice to establish a PATU-8988T xenograft model[1].
Dosage: 15 mg/kg, 50 mg/kg
Administration: I.p., once every two days (three times) or once
Result: Significant FAK degradation was induced in the spleen, liver, and lung tissues after 24 hours.
FAK protein levels partially recovered, but the degradation effect persisted (especially in the spleen and liver).
分子量

955.03

Formula

C50H57F3N8O8
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

BSJ-04-146 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:

BSJ-04-1462414478-45-6PROTACsFAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseFocal Adhesion KinasePROTACpancreatic cancertriple-negative breast cancerTNBCInhibitorinhibitorinhibit

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产品名称：
BSJ-04-146
目录号：
HY-179512
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