1. Metabolic Enzyme/Protease
    Apoptosis
  2. Mitochondrial Metabolism
    Apoptosis
  3. IACS-010759

IACS-010759 (Synonyms: IACS-10759)

製品番号: HY-112037 純度: 99.60%
取扱説明書

IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.

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IACS-010759 構造式

IACS-010759 構造式

CAS 番号 : 1570496-34-2

容量 価格(税別) 在庫状況 数量
Solution
10 mM * 1 mL in DMSO USD 186 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 186 在庫あり
Estimated Time of Arrival: December 31
Solid
5 mg USD 150 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 220 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 450 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 650 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 950 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

IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research[1][2].

IC50 & Target

OXPHOS[1]

体外実験

IACS-010759 (10, 30, 100 nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML[1].
IACS-010759 (0.001, 0.01, 0.1, 1, 10, 100, 1000 nM; 72 hurs) robustly inhibits both OCR and galactose-dependent H460 cell viability and has nearly identical IC50 values of 1.4 nM[1].
IACS-010759 is similarly active in mouse (average IC50 = 5.6 nM), rat (IC50 = 12.2 nM), and cynomolgus monkey (IC50 = 8.7 nM) cell lines[1].
IACS-010759 (0.01-10 μM) yieldes a maximal reduction of growth of > 50% in the majority of cancer cell lines (24 of 30 pancreatic (PDAC), 19 of 20 ovarian, 13 of 16 triple-negative breast (TNBC), 8 of 10 non-small-cell lung (NSCLC)) and a subset (11of 30 PDAC, 10 of 20 ovarian, 5 of 16 TNBC, 2 of 10 NSCLC) exhibited > 100% growth inhibition[1].

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

体内実験

IACS-010759 (5, 10, 25 mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10 mg/kg dose in mice bearing NB-1 (PGD-null) subcutaneous xenografts. IACS-010759 at the 25 mg/kg dose is not tolerated[1].
IACS-010759 HCl (10 mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent[1].
IACS-010759 (0.3 mg/kg for iv; 1 mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24 h)[1].

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

臨床実験
分子量

562.56

分子式

C25H25F3N6O4S

CAS 番号
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 : 62.5 mg/mL (111.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7776 mL 8.8879 mL 17.7759 mL
5 mM 0.3555 mL 1.7776 mL 3.5552 mL
10 mM 0.1778 mL 0.8888 mL 1.7776 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: 2.08 mg/mL (3.70 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

*All of the co-solvents are available by MCE.
参考文献

純度: 99.60%

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製品名:
IACS-010759
製品番号:
HY-112037
数量:
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