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GNE-1858

Cat. No. M9766
GNE-1858 Structure
Size Price Availability
5mg USD 447  USD447 Custom Synthesis
10mg USD 745  USD745 Custom Synthesis
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Quality Control & Documentation
Biological Activity

GNE-1858 is a potent, and ATP-competitive inhibitor of hematopoietic progenitor kinase-1 (HPK1). GNE-1858 against wild-type and active mimetic mutants HPK1-TSEE and HPK1-SA with IC50 values of 1.9 nM, 1.9 nM and 4.5 nM, respectively. Hematopoietic progenitor kinase-1 (HPK1) is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function.

Chemical Information
Molecular Weight 428.48
Formula C21H26F2N8
CAS Number 2680616-96-8
Solubility (25°C) DMSO ≥ 10 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] Ping Wu, et al. Structure. Hematopoietic Progenitor Kinase-1 Structure in a Domain-Swapped Dimer

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