1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Derazantinib

Derazantinib (Synonyms: ARQ-087)

製品番号: HY-19981 純度: 99.06%
取扱説明書

Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.

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Derazantinib 構造式

Derazantinib 構造式

CAS 番号 : 1234356-69-4

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 359 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 228 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 348 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 540 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 1080 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1680 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2880 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Derazantinib:

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FGFR アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.

IC50 & Target[1]

FGFR1

4.5 nM (IC50)

FGFR2

1.8 nM (IC50)

FGFR3

4.5 nM (IC50)

体外実験

In cells, inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) is evident by the response to Derazantinib treatment. Cell proliferation studies demonstrate Derazantinib has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein show a positive relationship between Derazantinib induced G1 cell cycle arrest and subsequent induction of apoptosis[1]. Derazantinib rescues the FGF2-mediated growth arrest with EC50 at about 100 nM, with no significant toxicity detected for up to 500 nM. The concentration range at which Derazantinib significantly suppresses the FGF2 effect is between 70-500 nM. Derazantinib inhibits FGF-mediated loss of extracellular matrix and induction of chondrocyte premature senescence. Derazantinib rescues FGF-mediated inhibition of chondrocyte differentiation in tibia cultures. Derazantinib inhibits FGFR1-4 but no other receptor tyrosine kinases in cell-free kinase assay. Derazantinib inhibits FGFR1 and FGFR2 mutants associated with craniosynostoses. Derazantinib rescues FGFR-mediated bone differentiation in mouse limb bud micromass cultures and ex vivo mouse calvarial organ cultures[2].

体内実験

Derazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions[1]. Most of the embryos exhibit abnormal external phenotype (81.3%) in Derazantinib-injected wings, possibly due to inhibition of proliferation of limb bud mesenchyme. The wings are shorter and thinner, with skeletal phenotype typical for FGFR inhibition, where ulna and radius are shorter or smaller in size, or occasionally missing completely[2].

臨床実験
分子量

468.57

分子式

C₂₉H₂₉FN₄O

CAS 番号

1234356-69-4

SMILES

COCCNCCC1=CC(NC2=NC=C3C[[email protected]@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 25 mg/mL (53.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1342 mL 10.6708 mL 21.3415 mL
5 mM 0.4268 mL 2.1342 mL 4.2683 mL
10 mM 0.2134 mL 1.0671 mL 2.1342 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
キナーゼ実験
[1]

Derazantinib is titrated in DMSO utilizing a 3-fold dilution scheme, and then diluted 10-fold further in deionized water for a final DMSO concentration of 10%. A volume (2.5 μL) of these dilutions or vehicle is added to each well of a reaction plate. FGFR1 or FGFR2 is added to assay buffer to each well in a volume of 17.5 μL for a final concentration of 0.50 or 0.25 nM, respectively. After a 30-minute pre-incubation period, ATP and substrate are added in assay buffer (5 μL) for final concentrations of 0-1,000 μM ATP and 80 nM biotinylated-PYK2, for a final reaction volume of 25 μL. The plates are incubated for 60 minutes at room temperature, and then stopped in the dark by the addition of 10 μL stop/detection mixture prepared in assay buffer containing EDTA[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

細胞実験
[1]

Cells are seeded at 3000-5000 cells per well with 130 μL media in 96-well tissue culture treated plates. The cells are incubated overnight and subsequently treated with 3-fold serial dilutions of Derazantinib starting at 100 μM. The cells are returned to a 37°C humidified incubator for 72 hours. Cell proliferation is measured using MTS assay[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[1]

Mice: Female NCr nu/nu mice (SNU-16) or CB17 SCID mice (NCI-H716) with well established (400 mg) subcutaneous tumors are given a single oral dose of Derazantinib or vehicle control. Plasma and tumor samples are collected 4 hours post single dose. Derazantinib is administered orally. Dosing volume for all groups is 10 mL/kg or 0.1 mL/10 g body weight[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

DerazantinibARQ-087ARQ087ARQ 087FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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製品名:
Derazantinib
製品番号:
HY-19981
数量:
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