XL 388
XL388
CAS: 1251156-08-7
Molecular Formula: C23H22FN3O4S
XL 388 - Names and Identifiers
XL 388 - Physico-chemical Properties
| Molecular Formula | C23H22FN3O4S |
| Molar Mass | 455.5 |
| Density | 1.354±0.06 g/cm3(Predicted) |
| Melting Point | >188oC (dec.) |
| Boling Point | 738.6±60.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Off-White to Pale Yellow |
| pKa | 6.22±0.13(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Stability | Hygroscopic |
| In vitro study | In MCF-7 cells, XL388 inhibited the phosphorylation of p70S6K by mTORC1 (T389) with an IC50 of 94 nM. XL388 inhibits phosphorylated AKT of mTORC2 (S473) with an IC50 of 350 nM. In vitro, XL388 inhibited the activity of solid and hematopoietic tumor cell lines and MCF-7 cell line proliferation (IC50 of 1.37 μm). XL388 and the chemotherapeutic drug act synergistically to prevent cell viability in a cellular assay. |
| In vivo study | When administered orally once daily to mice, XL388 exhibited anti-cancer activity in multiple xenograft models, including> 100% anti-tumor activity in the xenograft model MCF-7. XL388 demonstrated good pharmacokinetics and oral exposure in multiple species with moderate bioactivity. Mean plasma protein binding was 86%,90%,89%,85% and 84% as assessed with 5 μm XL388 in humans, monkeys, dogs, rats and mice, respectively. Oral administration of XL388 demonstrated significant and dose-dependent antitumor activity in human tumor xenografted athymic nude mice. Strong inhibition of mTORC1 and mTORC2 was achieved at 100 mg/kg XL388 for 4-8 hours. After 4-8 hours of oral administration, phosphorylation of target AKT(T308) of PI3K appeared to be moderately inhibited (39-45%). |
XL 388 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.195 ml | 10.977 ml | 21.954 ml |
| 5 mM | 0.439 ml | 2.195 ml | 4.391 ml |
| 10 mM | 0.22 ml | 1.098 ml | 2.195 ml |
| 5 mM | 0.044 ml | 0.22 ml | 0.439 ml |
Last Update：2024-01-02 23:10:35
XL 388 - Reference Information
| biological activity | XL388 is a highly effective, ATP-competitive mTOR selective inhibitor with IC50 of 9.9 nM, which is 1000 times higher than the selectivity of closely related PI3K kinase. |
| target | TargetValue mTORC1 () 8 nM mTOR 9.9 nM mTORC2 166 nM |
| Target | Value |
| mTORC1 () | 8 nM |
| mTOR | 9.9 nM |
| mTORC2 | 166 nM |
| in vitro study | in MCF-7 cells, XL388 inhibited mTORC1 phosphorylation of p70S6K(T389),IC50 is 94 nM. XL388 inhibits phosphorylation of mTORC2 AKT(S473),IC50 is 350 nM. In vitro, XL388 inhibited the activity of solid and hematopoietic tumor cell lines and MCF-7 cell line proliferation (IC50 is 1.37 μM). XL388 and chemotherapeutic drugs act synergistically to block cell viability in cell assays. |
| In vivo studies | When given orally to mice once a day, XL388 showed anti-cancer activity in multiple xenograft models, including anti-tumor activity in MCF-7 xenograft models> 100%. XL388 showed good pharmacokinetics and oral contact in multiple species, and had moderate biological activity. Mean plasma protein binding was 86%,90%,89%,85% and 84%, as assessed with 5 μM XL388 in human, monkey, dog, rat and mouse, respectively. Oral XL388 showed significant and dose-dependent anti-tumor activity in human tumor xenograft athymic nude mice. The strong inhibitory effect on mTORC1 and mTORC2 was achieved at 100 mg/kg XL388 for 4-8 hours. After 4-8 hours of oral administration, the phosphorylation of target AKT(T308) of PI3K showed moderate inhibition (39-45%). |
Last Update：2024-04-09 20:45:29
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CAS: 1251156-08-7
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Product Name: XL388 Visit Supplier Webpage Request for quotation
CAS: 1251156-08-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1251156-08-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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