XL388

This product is for research use only, not for human use. We do not sell to patients.

XL388
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Size Price Stock
100mg$800Check With Us
250mg$1340Check With Us
500mg$2010Check With Us

Cat #: V0206 CAS #: 1251156-08-7 Purity ≥ 98%

Description: XL388 is a novel, highly potent, selective, oral, ATP-competitive inhibitor of mTOR (mammalian target of rapamycin) with potential antitumor activity.

References: Takeuchi CS, et al. Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). J Med Chem. 2013 Mar 28;56(6):2218-34.

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Molecular Weight (MW)455.50
Molecular FormulaC23H22FN3O4S
CAS No.1251156-08-7
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 23 mg/mL (50.5 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES CodeO=C(N1CCOC2=CC=C(C3=CC=C(N)N=C3)C=C2C1)C4=CC=C(S(=O)(C)=O)C(F)=C4C
SynonymsXL388; XL-388; XL 388
ProtocolIn VitroXL388 (Compound 28) also inhibits DNA-PK with an IC50 of 8.831 μM. XL388 inhibits cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. XL388 acts in an ATP-competitive manner, with a linear increase in IC50 values with increasing ATP concentration.
In VivoTo 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)).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1954 mL10.9769 mL21.9539 mL43.9078 mL
5mM0.4391 mL2.1954 mL4.3908 mL8.7816 mL
10mM0.2195 mL1.0977 mL2.1954 mL4.3908 mL
20mM0.1098 mL0.5488 mL1.0977 mL2.1954 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.