MZH29
MZH29 is a potent and orally active FLT3 inhibitor. MZH29 shows inhibitory effects on wild-type and mutant FLT3, including the FLT3-ITD, FLT3-D835H/Y/V and FLT3-K663Q mutants. MZH29 retains its potent inhibitory effect against the FLT3-ITD/F691L mutation, a drug resistance mutation against the well-known FLT3 inhibitor, AC220 (HY-13001). MZH29 can be used for the research of cancer, such as acute myeloid leukemia (AML).
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- CAS No.: 2089590-80-5
- 화학식: C31H33FN4O5
- 분자량:560.62
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.17 nM
Compound: 10; MZH29
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835H
Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835H
|
[PMID: 33719439] |
| BaF3 | IC50 |
0.19 nM
Compound: 10; MZH29
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835Y
Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835Y
|
[PMID: 33719439] |
| BaF3 | IC50 |
0.22 nM
Compound: 10; MZH29
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD
|
[PMID: 33719439] |
| BaF3 | IC50 |
1.1 nM
Compound: 10; MZH29
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-F691L
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-F691L
|
[PMID: 33719439] |
| BaF3 | IC50 |
2.5 nM
Compound: 10; MZH29
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835V
Antiproliferative activity against mouse BaF3 cells expressing FLT3-D835V
|
[PMID: 33719439] |
| BaF3 | IC50 |
22 nM
Compound: 10; MZH29
|
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD-D835Y
|
[PMID: 33719439] |
| MOLM-13 | IC50 |
0.24 nM
Compound: MZH29
|
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
|
[PMID: 32659083] |
| MOLM-14 | IC50 |
0.13 nM
Compound: 10; MZH29
|
Antiproliferative activity against human MOLM-14 cells
Antiproliferative activity against human MOLM-14 cells
|
[PMID: 33719439] |
| MV4-11 | IC50 |
0.14 nM
Compound: 10; MZH29
|
Cytotoxicity against human MV4-11 cells
Cytotoxicity against human MV4-11 cells
|
[PMID: 33719439] |
| MV4-11 | IC50 |
0.14 nM
Compound: MZH29
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
|
[PMID: 32659083] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2089590-80-5
-
분자량 560.62
-
화학식 C31H33FN4O5
-
SMILES
O=C(NC1=CC=CC(C)=C1)NC2=CC=C(OC3=CC=NC4=CC(OCCCN5CCOCC5)=C(OC)C=C34)C(F)=C2
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)