Free shipping on all orders over $ 500

MS4078

Cat. No. M9397
MS4078 Structure
Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 550  USD550 In stock
25mg USD 985  USD985 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

MS4078 is a PROTAC degrader of ALK which potently decreases cellular levels of oncogenic active ALK fusion proteins in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells, with a Kd of 19 nM for binding affinity to ALK. MS4078 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In NCI-H2228 cells, MS4078 reduces the EML4-ALK protein levels with similar DC50 value of 59 ± 16 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels

Chemical Information
Molecular Weight 914.47
Formula C45H52ClN9O8S
CAS Number 2229036-62-6
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] Zhang C, et al. Eur J Med Chem. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).

Related ALK Products
Conteltinib

Conteltinib (CT-707) is a potent second-generation mesenchymal lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with antitumor activity for studies related to hepatocellular carcinoma (HCC).

M4K2234 

M4K2234 (compound 26b) is an ALK2 inhibitor. M4K2234 inhibits ALK2 and ALK5 with IC50s of 5 and 2144 nM, respectively. M4K2234 can be used as a chemical probe for ALK1 and ALK2 protein kinases. M4K2234 can be used for the research of cancer.

ZX-29 

ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.

Ficonalkib 

Ficonalkib is a potent inhibitor of Anaplastic lymphoma kinase (ALK), the tyrosine kinase receptor. Ficonalkib, can be used as an antineoplastic agent.

Envonalkib citrate 

Envonalkib citrate is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib citrate can be used for the research of non-small cell lung cancer.

  Catalog
Abmole Inhibitor Catalog




Keywords: MS4078 supplier, ALK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.