DDO-2728 |
| Catalog No.GC73579 |
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3029515-97-4
Sample solution is provided at 25 µL, 10mM.
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DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N6 metladenosine (m6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research.
DDO-2728 (0-40 μM, 48 h) increases m6A metlation levels in the MOLM-13, HEK293and MV4−11 cells over a concentration gradient[1].DDO-2728 (0.01-100 μM, 72 h) inhibits the proliferation of MOLM-13 and MV4−11 cells with IC50s of 0.45 and 1.2 μM respectively, and showes a relatively weak toxicity in HEK293 and HUVECs[1].DDO-2728 (20 μM, 48 h) significantly arrests the cell cycle of MOLM-13 and MV4−11 cells at the G1/M phase[1].DDO-2728 (5, 10 μM, 48 h) concentration-dependently induces cell apoptosis of MV4−11 and MOLM-13 cells[1].DDO-2728 (20 μM, 24 h) decreases the half-lives of TACC3 mRNA in MOLM-13 and MV4−11 cells[1].DDO-2728 (0-10 μM, 48 h) significantly reduces the abundance of TACC3 and c-Myc in MOLM-13 and MV4−11 cells at both mRNA and protein levels[1].1.19Metabolic Stability in Rat and Human Plasma and Liver Microsomes[1]
DDO-2728 (10-40 mg/kg, i.p., daily for 14 d) effectively inhibits tumor growth in MV4−11 xenograft nude mice.[1].1.19Pharmacokinetic Parameters of DDO-2728 in Rats[1]
References:
[1]. Zheng-Yu Jiang, et al. Discovery of Pyrazolo[1,5-a]pyrimidine Derivative as a Novel and Selective ALKBH5 Inhibitor for the Treatment of AML. Journal of Medicinal Chemistry. 2023，Article ASAP.
| Cas No. | 3029515-97-4 | SDF | |
| Formula | C28H17F3N4O7 | M.Wt | 578.45 |
| Solubility | DMSO : 125 mg/mL (216.09 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7288 mL | 8.6438 mL | 17.2876 mL |
| 5 mM | 0.3458 mL | 1.7288 mL | 3.4575 mL |
| 10 mM | 0.1729 mL | 0.8644 mL | 1.7288 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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