Structure of Abexinostat
CAS No.: 783355-60-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
PCI-24781 is a pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.
Synonyms: Pci-24781; CRA 024781; CRA-24781
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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 783355-60-2 |
Formula : | C21H23N3O5 |
M.W : | 397.42 |
SMILES Code : | O=C(C1=C(CN(C)C)C2=CC=CC=C2O1)NCCOC3=CC=C(C(NO)=O)C=C3 |
Synonyms : |
Pci-24781; CRA 024781; CRA-24781
|
MDL No. : | MFCD10565969 |
InChI Key : | MAUCONCHVWBMHK-UHFFFAOYSA-N |
Pubchem ID : | 11749858 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
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In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
human CD34+ cells | 10 to 100 nM | 24 hours | Abexinostat inhibited CFU-MK growth, megakaryocyte (MK) proliferation and differentiation. These effects required only a short incubation period. | PMC3730430 |
human skeletal (mesenchymal) stem cells (hMSCs) | 500 nM | 24 hours | Abexinostat promoted adipocytic differentiation of hMSCs by inducing the expression of several proadipocytic genes and significantly increasing the enrichment of the H3K9Ac epigenetic mark on the promoter regions of AdipoQ, FABP4, PPARγ, KLF15, CEBPA, SP7, and ALPL. | PMC4954455 |
HCT116 colon cancer cells | 0.2 µM, 0.5 µM, 1.0 µM | 24 hours | To measure the effect of PCI-24781 on RAD51 protein levels, results showed a significant decrease in RAD51 protein levels by 24 hours. | PMC2148315 |
MDA-MB-231 | 30 μM | 48 h | To screen for epigenetic small molecule inhibitors with anti-tumor activity | PMC7797697 |
Ramos cells | 0.5 μM to 2.0 μM | 48 hours | PCI-24781 induced concentration-dependent apoptosis in Ramos cells with an IC50 of 0.5 μM | PMC2704489 |
SUDHL4 cells | 0.5 μM to 2.0 μM | 48 hours | PCI-24781 induced concentration-dependent apoptosis in SUDHL4 cells with an IC50 of 0.8 μM | PMC2704489 |
HF1 cells | 0.5 μM to 2.0 μM | 48 hours | PCI-24781 induced concentration-dependent apoptosis in HF1 cells with an IC50 of 0.9 μM | PMC2704489 |
L428 cells | 0.5 μM to 2.0 μM | 48 hours | PCI-24781 induced concentration-dependent apoptosis in L428 cells with an IC50 of 1.4 μM | PMC2704489 |
U87 | 0.5–1.25 μM | 48 hours | To evaluate the inhibitory effect of PCI-24781 on GBM cell proliferation, results showed that PCI-24781 significantly inhibited the proliferation of U87 cells. | PMC8543939 |
U251 | 0.5–1.25 μM | 48 hours | To evaluate the inhibitory effect of PCI-24781 on GBM cell proliferation, results showed that PCI-24781 significantly inhibited the proliferation of U251 cells. | PMC8543939 |
U-118MG | 0.5–1.25 μM | 48 hours | To evaluate the inhibitory effect of PCI-24781 on GBM cell proliferation, results showed that PCI-24781 significantly inhibited the proliferation of U-118MG cells. | PMC8543939 |
DRAA8/CHO cells | 2.0 µM, 3.0 µM | 6 hours | To determine the effect of PCI-24781 on homologous recombinational repair, results showed that 2.0 μM and 3.0 μM PCI-24781 reduced the recombination frequency to 0.27% and 0.16%, respectively. | PMC2148315 |
MDA-MB-231 | 3 μM | 72 h | To screen for inhibitors that can kill cancer cells with high efficiency | PMC7797697 |
MDA-MB-231 | 0.3 μM and 0.15 μM | 72 h | To explore the most effective inhibitor at a low dose | PMC7797697 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Nude mice | MDA-MB-231 xenograft model | intravenous injection | 50 mg/kg | every other day for four weeks | To evaluate the anti-tumor effect of PCI-24781 in vivo | PMC7797697 |
BALB/c Nude mice | HCT116 colon cancer xenograft model | Oral | 200 mg/kg | 1×, 2×, or 3× over 4, 22, and 28 hours, respectively | To examine the effect of PCI-24781 on RAD51 protein levels in tumors, results showed a 69% decrease in RAD51 protein levels after 3 doses over 28 hours. | PMC2148315 |
Rats | Sprague-Dawley rats | Oral | 8.00 mg/kg | Single dose | To study the pharmacokinetic properties of Abexinostat in rats, the results showed that after oral administration, the absorption was rapid, the maximum plasma concentration (Cmax) was 28.20 ± 7.67 ng/mL, the time to peak (Tmax) was about 1.39 ± 1.29 h, and the half-life (t1/2) was 13.80 ± 2.50 h. | PMC10877774 |
Mice | GBM mouse model | Oral | 12.5 mg/kg BW | BID, 5 days a week for 4 weeks | To evaluate the inhibitory effect of PCI-24781 on GBM tumor growth in vivo, results showed that PCI-24781 significantly reduced tumor burden and increased survival. | PMC8543939 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT03934567 | Lymphoma, Follicular | PHASE2 | RECRUITING | 2024-09-30 | Cancer Hospital Chinese Academ... More >>y of Medical Sciences, Beijing, 100021, China|China-Japan Friendship Hospital, Beijing, 100029, China|Peking University Third Hospital, Beijing, 100191, China|Jilin Cancer Hospital, Changchun, 130012, China|West China Hospital, Sichuan University, Chengdu, 610041, China|The First Affiliated Hospital of Dalian Medical University, Dalian, 116011, China|Fujian Medical University Union Hospital, Fuzhou, 350001, China|Cancer Center of Guangzhou Medical University, Guangzhou, 510030, China|Sun Yai-Sen Memorial Hospital, Sun Yai-Sen University, Guangzhou, 510120, China|Nanfang Hospital, Guangzhou, 510515, China|Hainan General Hospital, Hainan, 570311, China|The Second Affiliated Hospital Zhejiang University School of Medicine, Hangzhou, 310009, China|Sir Run Run Shaw Hospital, Zhejiang University School of Medical, Hangzhou, 310020, China|Zhejiang Cancer Hospital, Hangzhou, 310022, China|The Affiliated Tumor Hospital of Harbin Medical University, Harbin, 150081, China|The First Hospital of Lanzhou University, Lanzhou, 730000, China|Linyi Cancer Hospital, Linyi, 276000, China|Nantong Tumor Hospital, Nantong, 226361, China|Shanghai Sixth people's hospital, Shanghai, 200025, China|Fudan University Shanghai Cancer Center, Shanghai, 200032, China|The Forth Hospital of Hebei Medical University, Shijiazhuang, 050011, China|Tianjin People's Hospital, Tianjin, 300000, China|Tianjin Medical University General Hospital, Tianjin, 300052, China|The Affiliated Hospital of Xuzhou Medical University, Xuzhou, 221006, China|Henan Cancer Hospital, Zhengzhou, 450008, China|The First Affiliated Hospital of Zhengzhou University, Zhengzhou, 450052, China Less << |
NCT04024696 | Non Hodgkin Lymphoma | PHASE1|PHASE2 | ACTIVE_NOT_RECRUITING | 2024-06-30 | Cancer Hospital Chinese Academ... More >>y of Medical Sciences, Beijing, 100021, China|Zhejiang Cancer Hospital, Hangzhou, 310022, China|Tianjin Medical University General Hospital, Tianjin, 300052, China|The Affiliated Hospital of Xuzhou Medical University, Xuzhou, 221006, China Less << |
NCT03600441 | Follicular Lymphoma | PHASE2 | ACTIVE_NOT_RECRUITING | 2025-12-31 | Advocate Medical Group - Park ... More >>Ridge, Luther Lane - Oncology, Park Ridge, Illinois, 60068, United States|Norton Cancer Institute - St. Matthews Campus, Louisville, Kentucky, 40207, United States|Clinical Research Alliance Inc, Lake Success, New York, 11042, United States|Manhattan Hematology Oncology Center, New York, New York, 10016, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Bone Marrow Transplant Hematology Oncology Associates, Pittsburgh, Pennsylvania, 15224-2156, United States|Arlington Cancer Center, Arlington, Texas, 76012, United States|Central Texas Veterans Health Care System - NAVREF, Temple, Texas, 76504, United States|Vista Oncology Inc. PS, Olympia, Washington, 98506, United States|Centre Hospitalier de Perpignan, Perpignan, Pyrénées-Orientales, 66046, France|Hospital Universitario de Donostia, Donostia-San Sebastián, Guipúzcoa, 20014, Spain|Hospital Universitario Vall d'Hebrón, Barcelona, 08035, Spain|Hospital del Mar, Barcelona, 28229, Spain|C.H. Regional Reina Sofia, Córdoba, 14004, Spain|Hospital Universitario Infanta Leonor, Madrid, 28031, Spain Less << |
NCT00473577 | Hematologic Neoplasms|Neoplasm... More >>s Less << | PHASE1 | COMPLETED | 2025-12-07 | University of Chicago, Chicago... More >>, Illinois, 60643, United States Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.16mL 5.03mL 2.52mL |
|
Dissolving Methods |
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
|
Tags: Abexinostat | CRA 024781 | PCI-24781 | CRA024781 | CRA-024781 | PCI24781 | PCI 24781 | PCI-24781 | HDAC Inhibitor | Histone deacetylases | MBLAC2 Inhibitor | antitumor activity | metallo-β-lactamase domain-containing protein 2 | 783355-60-2
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