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A-770041

Cat. No. M14910
A-770041 Structure
Size Price Availability
5mg USD 290  USD290 1-2 Weeks
10mg USD 460  USD460 1-2 Weeks
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Quality Control & Documentation
Biological Activity

A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling. IC50 value: 147 nM Target: Lck

Chemical Information
Molecular Weight 621.73
CAS Number 869748-10-7
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] Jonas Weie, et al. Identification of lymphocyte cell-specific protein-tyrosine kinase (LCK) as a driver for invasion and migration of oral cancer by tumor heterogeneity exploitation

[2] Li Li, et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1

[3] Zhenfeng Duan, et al. A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells

[4] Andrew Burchat, et al. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection

[5] Robert F Stachlewitz, et al. A-770041, a novel and selective small-molecule inhibitor of Lck, prevents heart allograft rejection

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