1. Epigenetics
    TGF-beta/Smad
  2. PKC

VTX-27 

目录号: HY-112782
产品使用指南

VTX-27 是蛋白激酶 C θ (PKC θ) 的选择性抑制剂,其对 PKC θ 和 PKC δ 的 Ki 值分别为 0.08 nM 和 16 nM。

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VTX-27 Chemical Structure

VTX-27 Chemical Structure

CAS No. : 1321924-70-2

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥4792 In-stock
2 mg ¥2600 In-stock
5 mg ¥5200 In-stock
10 mg ¥8500 In-stock
25 mg ¥17500 In-stock
50 mg ¥27500 In-stock
100 mg ¥39500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.

IC50 & Target[1]

PKCθ

0.08 nM (Ki)

PKCδ

16 nM (Ki)

PKCα

356 nM (Ki)

In Vitro

VTX-27 (Compound 27) possesses excellent overall characteristics. Good selectivity of VTX-27 is also seen against other PKC family members, particularly classical isoforms (>1000-fold except PKCβ I, 200-fold) and atypical isoforms (>10000-fold). As anticipated, attaining selectivity over the more closely related novel PKC family members is more challenging, with a good 200-fold being achieved over PKC δ[1].

In Vivo

VTX-27 shows the best PK profile with a low clearance (7 mL min-1 kg-1), long half-life (4.7 h), and good oral bioavailability (65%). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL) and demonstrates potent dose dependent inhibition of IL-2 production[1].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (298.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3872 mL 11.9360 mL 23.8720 mL
5 mM 0.4774 mL 2.3872 mL 4.7744 mL
10 mM 0.2387 mL 1.1936 mL 2.3872 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.97 mM); Clear solution

References
Molecular Weight

418.90

Formula

C₂₀H₂₄ClFN₆O

CAS No.

1321924-70-2

SMILES

FC1=C(N=C(N2C[C@@](NCC2)([H])[C@](C)(O)C(C)C)C(Cl)=C1)C3=NNC4=NC=CC=C34

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • 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)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Inquiry Information

产品名称:
VTX-27
目录号:
HY-112782
需求量:

VTX-27

Cat. No.: HY-112782