2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. BGB-8035

BGB-8035 是一种口服有效，高选择性 BTK 抑制剂，对 BTK、TEC、EGFR 的 IC50 分别为 1.1 nM、99 nM、621 nM。BGB-8035 具有抗肿瘤和抗关节炎活性。BGB-8035 具有用于 B 细胞恶性肿瘤和自身免疫性疾病研究的潜力。

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BGB-8035 Chemical Structure

BGB-8035 Chemical Structure

CAS No. : 2283349-24-4

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BGB-8035 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

BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research[1].

IC50 & Target

IC50: 1.1 nM (BTK), 99 nM (TEC), and 621 nM (EGFR)[1]
体外研究
(In Vitro)

BGB-8035 对 HEK293 和 Ramos 细胞基本无毒 (IC50>10 μM)[1]。

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

BGB-8035 相关抗体:
体内研究
(In Vivo)

BGB-8035 (7.5, 15, 30 mg/kg; 灌胃给药; 每天两次; 16 天) 表现出剂量依赖性抗肿瘤活性[1]。
BGB-8035 (1, 3, 10, 30 mg/kg; 灌胃给药; 每天两次; 13 天) 在 8-9 周大的 Lewis 大鼠CIA 模型中以剂量依赖的方式抑制关节炎，并防止 CIA 模型相关的体重减轻[1]。
Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs[1].

Rats (IV; 1 mg/kg) Rats (PO; 5 mg/kg) Dogs (IV; 1 mg/kg) Dogs (PO; 2.5 mg/kg)
T1/2 (h) 1.0 2.5
CL (mL/min/kg) 24.4 6.89
Vss (L/kg) 0.9 0.74
Tmax (h) 0.25 0.42
Cmax (ng/mL) 667 1246
AUCinf (h∗ng/mL) 964 2645
F (%) 26.4 43

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

Animal Model: Female NOD/SCID mice at 9 weeks of age with REC-1 MCL xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; BID; 16 days
Result: Demonstrated dose-dependent antitumor activity, with TGI values of 64.1, 73.6, and 79.9%, respectively.
分子量

453.53

Formula

C24H31N5O4
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

BGB-8035 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

BGB-80352283349-24-4BGB8035BGB 8035BtkBruton tyrosine kinaseOrallybruton's tyrosine kinaseTECEGFRantitumorarthritisB-cell malignanciesautoimmuneInhibitorinhibitorinhibit

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目录号：
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