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GNF-2

Cat. No. M2571
GNF-2 Structure
Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 125  USD125 In stock
25mg USD 265  USD265 In stock
50mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.

Chemical Information
Molecular Weight 374.32
Formula C18H13F3N4O2
CAS Number 778270-11-4
Solubility (25°C) DMSO 60 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] Gyun Jee Song, et al. A Bcr-Abl Inhibitor GNF-2 Attenuates Inflammatory Activation of Glia and Chronic Pain

[2] Federico Rossari, et al. Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy

[3] Margaret J Clark, et al. GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein

[4] Hyun-Ju Kim, et al. The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity

[5] Mamduh Khateb, et al. Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism

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Keywords: GNF-2 supplier, Src-bcr-Abl, inhibitors, activators


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