TG100713

Catalog No.S2870

TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.

Price Stock Quantity  
USD 170 In stock
USD 570 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

TG100713 Chemical Structure

TG100713 Chemical Structure
Molecular Weight: 254.25

Validation & Quality Control

Cited by 1 publications:

1 customer reviews :

Quality Control & MSDS

Related Compound Libraries

TG100713 is available in the following compound libraries:

Product Information

  • Compare PI3K
    Compare PI3K Products
  • Research Area

Product Description

Biological Activity

Description TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
Targets PI3Kδ [1] PI3Kγ [1] PI3Kα [1] PI3Kβ [1]
IC50 24 nM 50 nM 165 nM 215 nM
In vitro TG 100713 also strongly inhibits EC proliferation. [1]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Kinase Assays PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services.

Cell Assay: [1]

Cell lines HUVEC
Concentrations 10 μM
Incubation Time 24, 48, 72 h
Method Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers are quantified by XTT assay.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Doukas J et al. Proc Natl Acad Sci U S A, 2006, 103(52), 19866-19871.

Chemical Information

Download TG100713 SDF
Molecular Weight (MW) 254.25
Formula

C12H10N6

CAS No. 925705-73-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 2 mg/mL (7.86 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Phenol, 3-(2,4-diamino-6-pteridinyl)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related PI3K Products

  • GDC-0032

    GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147)

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • LY294002

    LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation.

  • CAL-101 (Idelalisib, GS-1101)

    CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

  • Wortmannin

    Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

  • BEZ235 (NVP-BEZ235, Dactolisib)

    BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.

  • BKM120 (NVP-BKM120, Buparlisib)

    BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.

Recently Viewed Items

Tags: buy TG100713 | TG100713 supplier | purchase TG100713 | TG100713 cost | TG100713 manufacturer | order TG100713 | TG100713 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us