Free shipping on all orders over $ 500

X-376

Cat. No. M1743
X-376 Structure
Size Price Availability Quantity
2mg USD 110  USD110 In stock
5mg USD 230  USD230 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitors (TKIs) with IC50 of 0.61 nM. In Ambit kinome screens, cell growth inhibition studies, and surrogate kinase assays, X-376 was more potent inhibitors of ALK but less potent inhibitors of MET compared to PF-02341066. X-376 displayed potent antitumor activity in vivo with favorable pharmacokinetic and toxicity profiles.

Product Citations
Customer Product Validations & Biological Datas
Source Munich Industrial University (2018). Figure 36. X-376 (AbMole BioScience)
Method Kinase binding of small molecule inhibitors
Cell Lines BT-474 cells, Caki-1 cells, KM-12 and HEK-293 cells
Concentrations 1 μM
Incubation Time 24 h
Results Notably, the photosensitizing effect of small molecule inhibitors can also be used for photodynamic therapy of cancer.
Source Science (2017). Figure 4. X-376 (Abmole Bioscience)
Method Cell viability and proliferation assays
Cell Lines A-431 and ACHN cells
Concentrations 50 nM
Incubation Time 72 h
Results Regardless of whether or not EGFR carried an activating mutation, the combination was always more effective in inhibiting cell viability and proliferation than any one drug alone.
Chemical Information
Molecular Weight 547.41
Formula C25H25Cl2FN6O3
CAS Number 1365267-27-1
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Lovly CM et al. Cancer Res. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors.

Related ALK Products
NVL-655 TFA

NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC).

NVL-655

NVL-655 (ALK-IN-27) is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. NVL-655 (ALK-IN-27) can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC).

APG-2449

APG-2449 is an orally active, potent ALK/ROS1/FAK inhibitor with anti-tumor activity in a mouse model of non-small cell lung cancer (NSCLC).

ALK2-IN-5

ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor.

J-1048

J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor.

  Catalog
Abmole Inhibitor Catalog




Keywords: X-376 supplier, ALK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.