2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. HBC-12551

HBC-12551 是一种具有口服活性的 BTK 抑制剂 (HEK293 细胞中 IC50：BTK 为 1.31 nM；BTKC481S 为 2.18 nM)。HBC-12551 对弥漫性大 B 细胞淋巴瘤具有抗肿瘤活性。

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HBC-12551

HBC-12551 Chemical Structure

CAS No. : 2963606-11-1

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HBC-12551 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTKC481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma[1].

体外研究
(In Vitro)

HBC-12551 在 HEK293 细胞中可强效抑制 BTK 的磷酸化 (IC50 = 1.31 nM)，以及 BTKC481S 突变体的磷酸化 (IC50 = 2.18 nM)[1]。
HBC-12551 (72 h) 可强效降低恶性 B 细胞系 TMD8 (IC50 = 1.40 nM)、TMD8-BTK-C481S (IC50 = 1.92 nM)、OCI-Ly10 (IC50 = 1.86 nM) 和 REC-1 (IC50 = 3.11 nM) 在孵育 72 h 后的细胞活力[1]。
HBC-12551 ( 30 min) 可强效抑制人外周血单个核细胞 (PBMCs) 中 B 细胞活化，对 CD69 表达的 IC50 为 0.95 nM[1]。

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

HBC-12551 相关抗体:
体内研究
(In Vivo)

HBC-12551 (10-20 mg/kg；口服；每日一次；14 天) 在 TMD8 异种移植模型中表现出强效的剂量依赖性肿瘤生长抑制作用[1]。

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

Animal Model: CB17 SCID (female)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; QD; 14 days
Result: Inhibited tumor growth by 97.2% relative to vehicle control.
Resulted in tumor regression with a tumor growth inhibition (TGI) of 112.8%.
Showed no abnormal clinical observations or significant body weight loss in treated mice.
分子量

660.74

Formula

C34H41FN8O5
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

HBC-12551 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:

HBC-125512963606-11-1HBC12551HBC 12551BtkBruton tyrosine kinasehuman PBMCsB-cell lymphoma cellsOCI-Ly10BTKTyr223REC-1C481S mutant BTKHEK293 cellswild-type BTKTMD8Inhibitorinhibitorinhibit

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产品名称：
HBC-12551
目录号：
HY-181547
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