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UM-164

Cat. No. M20634
UM-164 Structure
Synonym:

DAS-DFGO-II

Size Price Availability Quantity
10mg USD 148  USD148 In stock
50mg USD 340  USD340 In stock
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Quality Control & Documentation
Biological Activity

UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.

Chemical Information
Molecular Weight 640.68
Formula C30H31F3N8O3S
CAS Number 903564-48-7
Solubility (25°C) DMSO 5 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] Huizhe Xu, et al. Cancers (Basel). UM-164, a Dual Inhibitor of c-Src and p38 MAPK, Suppresses Proliferation of Glioma by Reducing YAP Activity

[2] Umar Ndagi, et al. RSC Adv. An analogue of a kinase inhibitor exhibits subjective characteristics that contribute to its inhibitory activities as a potential anti-cancer candidate: insights through computational biomolecular modelling of UM-164 binding with lyn protein

[3] Rabia A Gilani, et al. Clin Cancer Res. Retraction: UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer

[4] Umar Ndagi, et al. Appl Biochem Biotechnol. Emergence of a Promising Lead Compound in the Treatment of Triple Negative Breast Cancer: An Insight into Conformational Features and Ligand Binding Landscape of c-Src Protein with UM-164

[5] Rabia A Gilani, et al. Clin Cancer Res. UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer

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Keywords: UM-164, DAS-DFGO-II supplier, Src-bcr-Abl, inhibitors, activators


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