Free shipping on all orders over $ 500

JAK2 Inhibitor V

Cat. No. M3735
JAK2 Inhibitor V Structure
Synonym:

NSC 42834, Z3

Size Price Availability Quantity
5mg USD 65  USD65 In stock
10mg USD 95  USD95 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Z3 (NSC 42834) selectively inhibited Jak2 kinase function with no effect on Tyk2 or c-Src kinase function. Z3 significantly inhibited proliferation of the Jak2-V617F-expressing, human erythroleukemia cell line, HEL 92.1.7. The Z3-mediated reduction in cell proliferation correlated with reduced Jak2 and STAT3 tyrosine phosphorylation levels as well as marked cell cycle arrest. Finally, Z3 (NSC 42834) inhibited the growth of hematopoietic progenitor cells isolated from the bone marrow of an essential thrombocythemia patient harboring the Jak2-V617F mutation and a polycythemia vera patient carrying a Jak2-F537I mutation.

Chemical Information
Molecular Weight 344.45
Formula C23H24N2O
CAS Number 195371-52-9
Solubility (25°C) DMSO 40 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] Atallah E, et al. Expert Rev Anticancer Ther. Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms.

[2] Sayyah J, et al. Curr Oncol Rep. Jak2 inhibitors: rationale and role as therapeutic agents in hematologic malignancies.

[3] Sayyah J, et al. Mol Cancer Ther. Z3, a novel Jak2 tyrosine kinase small-molecule inhibitor that suppresses Jak2-mediated pathologic cell growth.

Related JAK Products
A-005

A-005 is a potentially first-in-class, brain-penetrating TYK2 allosteric inhibitor for studies related to neuroinflammatory and neurodegenerative diseases.

Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9)

Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide corresponding to amino acids 475 to 491 of mouse JAK2.

JAK2/FLT3-IN-1 TFA

JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively.

ZT55

ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM.

ZM39923

ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: JAK2 Inhibitor V, NSC 42834, Z3 supplier, JAK, 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.