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  3. NSC781406

NSC781406 

Cat. No.: HY-100470 Purity: 99.55%
Handling Instructions

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

For research use only. We do not sell to patients.

NSC781406 Chemical Structure

NSC781406 Chemical Structure

CAS No. : 1676893-24-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

IC50 & Target[1]

PI3Kα

2 nM (IC50)

PI3Kγ

2.7 nM (IC50)

PI3Kβ

9.4 nM (IC50)

PI3Kδ

14 nM (IC50)

mTOR

5.4 nM (IC50)

In Vitro

NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines[1].

In Vivo

In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight[1].

Molecular Weight

627.68

Formula

C₂₉H₂₇F₂N₅O₅S₂

CAS No.

1676893-24-5

SMILES

FC1=CC(F)=CC=C1S(=O)(NC2=CC(C3=CC=C(N=CC=C4C#CCN5CCN(S(C)(=O)=O)CC5)C4=C3)=CN=C2OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (238.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5932 mL 7.9658 mL 15.9317 mL
5 mM 0.3186 mL 1.5932 mL 3.1863 mL
10 mM 0.1593 mL 0.7966 mL 1.5932 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

IC50 values for inhibition of the PI3K is measured. PI-103 is used as the reference compound. The compounds (NSC781406) are tested in duplicate for 10 concentrations, 100 nM or 500 nM as the top concentration. All reagents are diluted in kinase buffer.Three-fold, ten-point serial compound (NSC781406) dilutions are performed in kinase buffer[1].

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

Cell Assay
[1]

Cytotoxic effects are tested in the human lung adenocarcinoma cells A549, human colon cancer cells HCT-116, human breast cancer cells MDA-MB-231 and human hepatocellular carcinoma cells BEL-7404. These four tumor cells are diluted to a density of 40,000–50,000 cells/mL in logarithmic phase. After the cells are treated with compounds (NSC781406) for 72 h, MTT solution (5 mg/mL, 20 μL) is added another 4h at 37°C. IC50 values are determined by a nonlinear regression analysis[1].

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

Animal Administration
[1]

Mice: NSC781406 is orally administered once a day 30 mg/kg for 14 consecutive days or with sorafenib at 50 mg/kg. The relative tumor volume to vehicle-treated control mice is monitored[1].

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

References
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Keywords:

NSC781406NSC 781406NSC-781406PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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