- XL388
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- $38.00
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2026-07-27
- CAS:1251156-08-7
- Purity: 99.53%
- Supply Ability: 10g
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| Product Name: | XL-388 | | Synonyms: | Methanone, [7-(6-amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-;[7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone XL388;XL388, >=98%;(7-(6-Aminopyridin-3-yl)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)(3-fluoro-2-methyl-4-(methy;XL 388;XL388;XL-388;[7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone | | CAS: | 1251156-08-7 | | MF: | C23H22FN3O4S | | MW: | 455.5 | | EINECS: | | | Product Categories: | PI3K/Akt/mTOR;Akt;mTOR;PI3K;Inhibitors | | Mol File: | 1251156-08-7.mol |  |
| | XL-388 Chemical Properties |
| Melting point | >188oC (dec.) | | Boiling point | 738.6±60.0 °C(Predicted) | | density | 1.354±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | | solubility | DMSO (Slightly), Methanol (Slightly) | | pka | 6.22±0.13(Predicted) | | form | Solid | | color | Off-White to Pale Yellow | | Stability: | Hygroscopic | | InChI | 1S/C23H22FN3O4S/c1-14-18(5-7-20(22(14)24)32(2,29)30)23(28)27-9-10-31-19-6-3-15(11-17(19)13-27)16-4-8-21(25)26-12-16/h3-8,11-12H,9-10,13H2,1-2H3,(H2,25,26) | | InChIKey | LNFBAYSBVQBKFR-UHFFFAOYSA-N | | SMILES | Fc1c(ccc(c1C)C(=O)N2CCOc3c(cc(cc3)c4c[nH][c](cc4)=N)C2)[S](=O)(=O)C |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| | XL-388 Usage And Synthesis |
| Uses | XL388 is a highly potent, orally bioavailable, selective, ATP-competitive mammalian target of rapamycin (mTOR) inhibitor. XL388 has shown significant and dose-dependent antitumor activity in athymic nude mice implanted with human tumor xenografts. | | Biological Activity | XL388 is a potent, selective, orally bioavailable ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) with an IC50 of 9.9 nM for mTOR, 8 nM for mTORC1, 166 nM for mTORC2, and 1000-fold selectivity for mTOR over the closely related PI3K kinases and a panel of 141 protein kinases tested. XL388 blocked mTORC1 phosphorylation of p70S6K (T389) with an IC50 value of 94 nM and blocked mTORC2 phosphorylationof AKT (S473) with an IC50 value of 350 nM. XL388 showed complete tumor growth inhibition in mice bearing MCF-7 xenograft tumors. | | in vivo | To assess the pharmacodynamic effects of XL388 (Compound 28) on the mTOR pathway signaling, athymic nude mice bearing PC-3 prostate tumors are dosed orally at 100 mg/kg of XL388. Rapamycin is also administered intraperitoneally at 5 mg/kg as a reference. Plasma and tumor samples are collected at 1, 4, 8, 16, 24, and 32 h for XL388 and at 4 h for Rapamycin after dosing and homogenized with buffer. Tumor lysates from each animal (n=5) are then pooled for each group and analyzed by immunoblot for levels of phosphorylated p70S6K, S6, 4E-BP1, and AKT. XL388 has moderate terminal elimination half-life (t1/2=1.35 h, 0.45 h, 6.11 h and 0.86 h for mouse (10 mg/kg, iv), rat (3 mg/kg, iv), dog (3 mg/kg, iv), monkey (3 mg/kg, iv))[1]. | | IC 50 | mTOR: 9.9 nM (IC50); mTORC1; mTORC2; DNA-PK: 8.831 μM (IC50) |
| | XL-388 Preparation Products And Raw materials |
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