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BX-912

Cat. No. M2311
BX-912 Structure
Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 170  USD170 In stock
50mg USD 540  USD540 In stock
100mg USD 800  USD800 In stock
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Quality Control & Documentation
Biological Activity

BX912 is a selective potent PDK1 inhibitor with an IC50 of 12 nM. BX912 also inhibits other kinases such as ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 potently prevents PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 < 10 μM). BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP. BX912 promotes a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G2/M phase of the cell cycle. BX912 also potently inhibits the growth of HCT-116 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM.

Chemical Information
Molecular Weight 471.35
Formula C20H23BrN8O
CAS Number 702674-56-4
Solubility (25°C) DMSO 60 mg/mL
Ethanol 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] Yiguang Bai, et al. Effects of inhibiting PDK‑1 expression in bone marrow mesenchymal stem cells on osteoblast differentiation in vitro

[2] Saori Maegawa, et al. Phosphoinositide-dependent protein kinase 1 is a potential novel therapeutic target in mantle cell lymphoma

[3] Farha Naz, et al. Evaluation of human microtubule affinity-regulating kinase 4 inhibitors: fluorescence binding studies, enzyme, and cell assays

[4] Farha Naz, et al. Designing New Kinase Inhibitor Derivatives as Therapeutics Against Common Complex Diseases: Structural Basis of Microtubule Affinity-Regulating Kinase 4 (MARK4) Inhibition

[5] Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1

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  Catalog
Abmole Inhibitor Catalog




Keywords: BX-912 supplier, PDK1, inhibitors, activators


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