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LCH-7749944

Cat. No. M21035
LCH-7749944 Structure
Synonym:

GNF-PF-2356

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Biological Activity

LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.

Chemical Information
Molecular Weight 350.41
Formula C20H22N4O2
CAS Number 796888-12-5
Solubility (25°C) DMSO 70 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] Irene Ramos-lvarez, et al. Am J Physiol Gastrointest Liver Physiol. Group II p21-activated kinase, PAK4, is needed for activation of focal adhesion kinases, MAPK, GSK3, and β-catenin in rat pancreatic acinar cells

[2] Irene Ramos-Alvarez, et al. Am J Physiol Gastrointest Liver Physiol. Cyclic AMP-dependent protein kinase A and EPAC mediate VIP and secretin stimulation of PAK4 and activation of Na+,K+-ATPase in pancreatic acinar cells

[3] Irene Ramos-Alvarez, et al. Am J Physiol Gastrointest Liver Physiol. P21-activated kinase 4 in pancreatic acinar cells is activated by numerous gastrointestinal hormones/neurotransmitters and growth factors by novel signaling, and its activation stimulates secretory/growth cascades

[4] Q Guo, et al. Oncogene. PAK4 kinase-mediated SCG10 phosphorylation involved in gastric cancer metastasis

[5] Jian Zhang, et al. Cancer Lett. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells

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Keywords: LCH-7749944, GNF-PF-2356 supplier, PAK, inhibitors, activators

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