Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H12N2O2 |
Molecular Weight | 276.2894 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C(=O)\C(C2=C1C=CC=C2)=C3\C(=O)NC4=C3C=CC=C4
InChI
InChIKey=QNOCRUSVMMAKSC-CCEZHUSRSA-N
InChI=1S/C17H12N2O2/c1-19-13-9-5-3-7-11(13)15(17(19)21)14-10-6-2-4-8-12(10)18-16(14)20/h2-9H,1H3,(H,18,20)/b15-14+
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/25050545Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25151579 | https://www.ncbi.nlm.nih.gov/pubmed/20233051 | https://www.ncbi.nlm.nih.gov/pubmed/12685829
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25050545
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/25151579 | https://www.ncbi.nlm.nih.gov/pubmed/20233051 | https://www.ncbi.nlm.nih.gov/pubmed/12685829
Meisoindigo ((E)-1,1'-dimethyl-[3,3'-biindolinylidene]-2,2'-dione) is a derivative of Indigo Naturalis, that has been used in China for chronic myeloid leukemia. In vitro cell line studies have shown that this agent might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML). Meisoindigo has been a routine therapeutic agent in the clinical treatment of chronic myelogenous leukemia (CML) in China since the 1980s. In phase III clinical trial of Meisoindigo involving 402 patients, it was shown that Meisoindigo was equally efficient for both newly diagnosed and previously treated CML patients after oral administration. The hematological complete response (CR) and partial response (PR) rates, respectively, were 45.0 and 39.3% for newly diagnosed patients and 35.9 and 41.4% for previously treated patients. Meisoindigo was generally well tolerated. The most frequent
side‑effects were bone, joint and/or muscle pain of varying degrees when the dosage was more than the suitable one.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5698 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19783149 |
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Target ID: CHEMBL6003 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19783149 |
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Target ID: CHEMBL3055 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19783149 |
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Target ID: GO:0090592 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12685829 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25050545 |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
MEISOINDIGO plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
19.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25050545 |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
MEISOINDIGO plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12685829
50–200 mg/d
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25050545
NB4 (APL cells, M3 subtype according to FAB), NB4.007/6 (retinoic acid resistant cells developed through continuously culturing NB4 in the medium containing retinoic acid), HL60 (AML cells, M2 subtype according to FAB), and U937 (myelomonocytic leukemia cells, M5 subtype according to FAB) were used for activity evaluation. The inhibitory effects of meisoindigo on the four human leukemic cells were tested by treating the cells with meisoindigo at various concentrations (0, 1, 2, 4, 8, 12, 16, 20 μM). The cells were cultured in 24‑well plates. The number of the cells was counted by trypan blue exclusion method. The initial cell numbers (NB4, NB4.007/6, HL60 and U937) were 3x10^6 cell/ml. After incubation for 24, 48 and 72 h, the plates
were taken out and the number of viable cells was counted.
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92UIP6405R
Created by
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97207-47-1
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5479433
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MEISOINDIGO
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admin on Fri Dec 15 17:28:13 GMT 2023 , Edited by admin on Fri Dec 15 17:28:13 GMT 2023
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PRIMARY | Official Title: A Single-center, Single- and Multiple-Dose Phase 1 Study to Evaluate the Safety and Pharmacokinetics of TAK-114 in Healthy Adult Japanese and Caucasian Male SubjectsPurpose: The purpose of this study is to evaluate the safety and tolerability of TAK-114 following single and multiple ascending oral doses in healthy Japanese subjects. | ||
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DTXSID901025868
Created by
admin on Fri Dec 15 17:28:13 GMT 2023 , Edited by admin on Fri Dec 15 17:28:13 GMT 2023
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ACTIVE MOIETY