1. PI3K/Akt/mTOR
    Epigenetics
    Cell Cycle/DNA Damage
  2. PI3K
    Epigenetic Reader Domain
    DNA-PK
  3. SF2523

SF2523 

製品番号: HY-101146 純度: 97.32%
取扱説明書

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

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SF2523 構造式

SF2523 構造式

CAS 番号 : 1174428-47-7

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 131 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 160 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 260 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 520 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 810 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1100 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

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Based on 1 publication(s) in Google Scholar

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製品説明

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

IC50 & Target[1]

PI3Kα

34 nM (IC50)

PI3Kγ

158 nM (IC50)

BRD4 (BD1)

241 nM (IC50)

DNA-PK

9 nM (IC50)

mTOR

280 nM (IC50)

体外実験

SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. SF2523 treatment leads to the displacement of BRD4 from both MYCN promoter sites. SF2523 interacts robustly with the full-length BRD4 (Kd=140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (Kd=150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (Kd=710 nM). Comparison of binding affinities of SF2523 for BDs of other proteins reveal that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs[2].

体内実験

SF2523 treatment results in a significant reduction of tumor volume compared with control. Importantly, SF2523 shows no gross toxicity to the treated mice, as there is no notable change in body weight. Tumors from SF2523-treated mice have markedly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors[2].

分子量

371.41

分子式

C₁₉H₁₇NO₅S

CAS 番号

1174428-47-7

SMILES

O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(OCCO5)C5=C4

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 : ≥ 30 mg/mL (80.77 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6924 mL 13.4622 mL 26.9244 mL
5 mM 0.5385 mL 2.6924 mL 5.3849 mL
10 mM 0.2692 mL 1.3462 mL 2.6924 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 (6.73 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
動物実験
[2]

Mice: After 20 d of tumor implantation, mice are treated with either (i) 30 mg/kg of SF2523 formulated in 15% DMA+30% captisol, (ii) 30 mg/kg of JQ1 formulated in 30% captisol in combination with 30 mg/kg of BKM120 formulated in 15% ethanol+15% cremaphore, (iii) vehicle (15% ethanol+15% cremaphore, as control), or (iv) another vehicle (15% DMA+30% captisol, as control) five times a week, until tumors are removed on day 35[2].

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:

SF2523SF 2523SF-2523PI3KEpigenetic Reader DomainDNA-PKPhosphoinositide 3-kinaseDNA-dependent protein kinaseInhibitorinhibitorinhibit

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製品名:
SF2523
製品番号:
HY-101146
数量:
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