PI 3-Kinase Inhibitor (PI-103) B-0303
PI-103
CAS: 371935-74-9
Molecular Formula: C19H16N4O3
PI 3-Kinase Inhibitor (PI-103) B-0303 - Names and Identifiers
| Name | PI-103 |
| Synonyms | PI-103 PI-103HydrochlorideSalt PI 3-Kinase Inhibitor (PI-103) B-0303 3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol |
| CAS | 371935-74-9 |
PI 3-Kinase Inhibitor (PI-103) B-0303 - Physico-chemical Properties
| Molecular Formula | C19H16N4O3 |
| Molar Mass | 348.36 |
| Density | 1.409±0.06 g/cm3(Predicted) |
| Solubility | Soluble in DMSO (up to 40 mg/ml) |
| Appearance | White solid |
| Color | White |
| pKa | 9.06±0.10(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Use | PI-103 is a multi-target PI3K inhibitor, which has the best inhibitory effect on p110α, IC50 is 2 nM (slightly weaker inhibitory effect on p110β/δ/γ), mTORC1/2 and DNA-PK ,IC50 is 20 nM/83 nM and 8 nM respectively. |
| In vitro study | PI-103 potently inhibits the apamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. PI-103 is the third most targeted PI3K inhibitor. PI-103 Inhibits Constitutive and growth factor-induced activation of PI3K/Akt and mTORC1. In blast cells, particularly leukemic stem cells, PI-103 inhibits leukemic cell proliferation and colony formation of leukemic precursor cells, and induces mitochondrial apoptosis. PI-103 inhibits p110α more than 200-fold more than p110β. PI-103 also potently inhibits PI(3,4)P2 and PIP3 in adipocytes, and PIP3 in myotubes. Compared with The IC50 value of LY294002 inhibiting Akt phosphorylation, the IC50 value of PI-103 inhibiting Akt phosphorylation was 100 times lower. The PI-103 protects the animals from insulin-stimulated lowering of blood glucose. The combination of PI-103 and etoposide has the effect of enhancing apoptosis in blast cells and immature leukemia cells. |
| In vivo study | When the tumor reaches 50-100mm |
PI 3-Kinase Inhibitor (PI-103) B-0303 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.871 ml | 14.353 ml | 28.706 ml |
| 5 mM | 0.574 ml | 2.871 ml | 5.741 ml |
| 10 mM | 0.287 ml | 1.435 ml | 2.871 ml |
| 5 mM | 0.057 ml | 0.287 ml | 0.574 ml |
Last Update：2024-01-02 23:10:35
PI 3-Kinase Inhibitor (PI-103) B-0303 - Reference Information
| biological activity | PI-103 is a multi-target PI3K inhibitor, which has the best inhibitory effect on p110α, the IC50 is 2 nM (slightly less inhibitory effect on p110β/δ/γ) and also inhibits mTORC1/2 and DNA-PK, with IC50 of 20 nM/83 nM and 8 nM, respectively. PI-103 is a multi-target PI3K inhibitor, the IC50 for p110α/β/δ/γ in cell-free assay was 2 nM/3 nM/3 nM/15 nM, and the effect on mTOR/DNA-PK was small, the IC50 was 30 nM/23 nM. PI-103 can induce apoptosis of T cell lymphoma in mice. |
| characteristics | PI-103 was the first potent synthetic mTOR inhibitor. |
| Target | Value |
| p110α (Cell-free assay) | 2 nM |
| p110β (Cell-free assay) | 3 nM |
| p110δ (Cell-free assay) | 3 nM |
| p110γ (Cell-free assay) | 15 nM |
| DNA-PK (Cell-free assay) | 23 nM |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: PI-103 Visit Supplier Webpage Request for quotationCAS: 371935-74-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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