BX-912
Based on 7 publication(s) in Google Scholar
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.50%
- CAS No.: 702674-56-4
- 화학식: C20H23BrN8O
- 분자량:471.35
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- Protocol
- 순도&문서
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BX-912
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- MedComm (2020). 2025 Dec 8;6(12):e70492. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Cancer Sci. 2023 Dec;114(12):4691-4705. [Abstract]
- Cancer Med. 2026 Mar;15(3):e71645. [Abstract]
- Biomed Pharmacother. 2025 Dec:193:118716. [Abstract]
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Flow Cytometry
-
Apoptosis Analysis
-
WB
Biological Activity
IC50: 26 nM (PDK1)[1]
BX-912 promotes a block at the G2/M phase of the cell cycle in MDA-468 cells[1].
BX-912 binds to the ATP binding site of PDK1, and is 9-fold selective for PDK1 relative to PKA. BX-912 blocks PDK1 activity in PTEN-negative PC-3 cells. PTEN-negative PC-3 cells display constitutive activation of Akt which is reflected in high levels of the PDK1 product, phospho-Thr308-Akt[1].
BX-912 is identified in a coupled assay measuring PDK1- and PtdIns-3,4-P2-mediated Akt activation, which can detect inhibitors of PDK1, AKT2, or other steps critical for activation of AKT2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 702674-56-4
-
Appearance Solid
-
분자량 471.35
-
화학식 C20H23BrN8O
-
Color White to off-white
-
SMILES
BrC1=C(NCCC2=CNC=N2)N=C(NC3=CC(NC(N4CCCC4)=O)=CC=C3)N=C1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
MedComm (2020)
Integrated Multi-Omics Profiling to Characterize Molecular Subtypes and Reveal Potential Therapeutic Strategies for Colorectal Cancer. [Abstract]2025 Dec 8;6(12):e70492. PMID: 41377767 -
Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Cancer Sci
Triple targeting of RSK, AKT, and S6K as pivotal downstream effectors of PDPK1 by TAS0612 in B-cell lymphomas. [Abstract]2023 Dec;114(12):4691-4705. PMID: 37840379
BX-912 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4691-4705. [Abstract]
Growth inhibitory effect of BX‐912 on eight BCL‐derived cell lines. Cells were treated with various concentrations of BX‐912 for 48 h.
BX-912 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4691-4705. [Abstract]
Cell cycle distribution assay by measuring DNA content of untreated cells (Ctrl.) and cells treated with IC80 concentration of BX‐912 for 24 h.
BX-912 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4691-4705. [Abstract]
Assays for apoptosis by counterstaining with Annexin‐V (AV) (X‐axis) and propidium iodide (PI) (Y‐axis) using flow cytometry. Untreated cells and cells treated with IC80 concentration of BX‐912 for 24 or 48 h were analyzed.
BX-912 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4691-4705. [Abstract]
Cells were treated with BX‐912 at IC80 concentration for each cell line for 12 h. Intensities of the proteins of interest in treated cells (+) relative to those of untreated cells (−) were calculated using ImageJ and described as individual bands.
-
Cancer Med
Identification and Validation of cGAS-STING Pathway-Associated Predictive and Therapeutic Models for Esophageal Squamous Cell Cancer Patients via Artificial Intelligence and Multi-Omics. [Abstract]2026 Mar;15(3):e71645. PMID: 41731722 -
Biomed Pharmacother
Drug target proteome profiling identifies HES1-driven mitotic catastrophe in ovarian serous carcinoma. [Abstract]2025 Dec:193:118716. PMID: 41202420
용액&용해도
DMSO : ≥ 100 mg/mL (212.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1 and PtdIns-3,4-P2 mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contains: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μL of the assay mixture on Streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay can sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The cell lines MDA-468, MDA-453, HCT-116, U87-MG, U2OS, PC-3, B16F10, and MiaPaCa; LOX amelanotic human melanoma cells; and HeLa cells seeded at a low density (1,500-3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of BX-912 (1, 10, 100 and 1000 nM) in 1% DMSO and growth medium (final concentration of DMSO, 0.1%), followed by brief shaking. Treated cells are incubated for 72 h, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
-
Data Sheet (274 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1216 mL | 10.6078 mL | 21.2157 mL | 53.0391 mL |
| 5 mM | 0.4243 mL | 2.1216 mL | 4.2431 mL | 10.6078 mL | |
| 10 mM | 0.2122 mL | 1.0608 mL | 2.1216 mL | 5.3039 mL | |
| 15 mM | 0.1414 mL | 0.7072 mL | 1.4144 mL | 3.5359 mL | |
| 20 mM | 0.1061 mL | 0.5304 mL | 1.0608 mL | 2.6520 mL | |
| 25 mM | 0.0849 mL | 0.4243 mL | 0.8486 mL | 2.1216 mL | |
| 30 mM | 0.0707 mL | 0.3536 mL | 0.7072 mL | 1.7680 mL | |
| 40 mM | 0.0530 mL | 0.2652 mL | 0.5304 mL | 1.3260 mL | |
| 50 mM | 0.0424 mL | 0.2122 mL | 0.4243 mL | 1.0608 mL | |
| 60 mM | 0.0354 mL | 0.1768 mL | 0.3536 mL | 0.8840 mL | |
| 80 mM | 0.0265 mL | 0.1326 mL | 0.2652 mL | 0.6630 mL | |
| 100 mM | 0.0212 mL | 0.1061 mL | 0.2122 mL | 0.5304 mL |
BX-912 Related Classifications
HY-11005 Related Classifications
Powered by Bioz