2. Epigenetics
  3. Epigenetic Reader Domain
  4. BET-IN-12

BET-IN-12 是一种具有口服活性的 BET 抑制剂，对 BRD4 的 IC50 为 0.9 nM。

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BET-IN-12 Chemical Structure

BET-IN-12 Chemical Structure

CAS No. : 1800343-11-6

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BET-IN-12 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

BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].

IC50 & Target

0.9 nM (BRD4)[1]
体外研究
(In Vitro)

BET-IN-12 (compound 15) (24 hours) displays BRD4 and c-Myc inhibition, MM proliferation with IC50s values of 0.9 nM, 2.0 nM, and 6.0 nM, respectively[1].
BET-IN-12 (compound 15) (24 hours) has high oxidative stability across species and low glucuronidation across species, so that translate into low orally administered minimum efficacious doses (MEDs) [1].

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

BET-IN-12 相关抗体:
体内研究
(In Vivo)

BET-IN-12 (compound 15) is 100% oral bioavailability in mouse[1].
BET-IN-12 (compound 15) impairs the growth of established PDX tumors (TGI = 88%) at MED = 2 mg/kg (AUC = 4800 nM•h)[1].
pharmacokinetic (PK) profile[1]

dose (iv/po, mg/kg) CLp ((mL/min)/kg) Vd (L/kg) half-life (ie, h) F (%) AUC (po, nM.h)
mouse 1.0/3.0 4.2 1.4 3.4 100 25000
rat 1.0/5.0 18 2.9 4.1 74 6600
dog 0.1/0.3 13 5.8 7.6 73 550
monkey 0.1/0.3 4.3 1.3 4.0 85 1900

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

516.62

Formula

C30H29D3FN5O2
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

BET-IN-12 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:

BET-IN-121800343-11-6Epigenetic Reader DomainbromodomainBET inhibitorgene transcriptioncancercarbolineInhibitorinhibitorinhibit

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