Free shipping on all orders over $ 500

CZ415

Cat. No. M7563
CZ415 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 240 In stock
50mg USD 920 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: Inhibition of phosphorylation for both downstream targets results in 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT. The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 hours in stimulated human whole blood and the resulting IC50 is 226 nM. As a predictor for cardiotoxicity, the activity of CZ415 against the human cardiac ion channel hERG is assessed in a whole-cell patch-clamp assay in HEK293 cells resulting in an IC50 of 48 μM.

In vivo: CZ415 is a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model. For full characterization of CZ415 and to enable improved dose predictions, the pharmacokinetic (PK) profile is assessed in rat. PK and oral bioavailability are determined after of 1 mg/kg intravenous (iv) bolus and 3 mg/kg oral (po) administration. The observed plasma clearance, corresponding to 45% liver blood flow, suggests that sufficient levels of free compound are circulating in the animal over time. The oral uptake is rapid with a Tmaxmax of 0.5 h and bioavailability F = 44% indicates very good absorption from the gut.

Protocol
Cell Experiment
Cell lines HNSCC cell
Preparation method SCC-9 cells (1×104 per 10-cm dish) were originally plated in 0.5% agarose-containing complete medium. After applied CZ415 treatment of 10 days, the survival SCC-9 colonies were manually counted.
Concentrations 100 nM
Incubation time 72 h
Animal Experiment
Animal models nude mice bearing SCC-9 tumors
Formulation
Dosages 20 mg/kg
Administration gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 459.56
Formula C22H29N5O4S
CAS Number 1429639-50-8
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

Targeting mTOR by CZ415 Inhibits Head and Neck Squamous Cell Carcinoma Cells.
Xie J, et al. Cell Physiol Biochem. 2018;46(2):676-686. PMID: 29621758.

The mTOR Kinase Inhibitor CZ415 Inhibits Human Papillary Thyroid Carcinoma Cell Growth.
Li X, et al. Cell Physiol Biochem. 2018;46(2):579-590. PMID: 29617677.

Related mTOR Products
GNE-477

GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.

Zotarolimus

Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.

LY303511

LY303511 is a structural analogue of LY294002, which does not inhibit PI3K, increased homotypic GJIC.

Temsirolimus

Temsirolimus (CCI-779) is a specific mTOR inhibitor with IC50 of 1.76 μM.

WYE-125132

WYE-125132 is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CZ415 supplier, mTOR, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.