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Cat. No.: HY-115443

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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).

For research use only. We do not sell to patients.

CAS No.: 2089590-80-5
Formula: C₃₁H₃₃FN₄O₅
Molecular Weight:560.62

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (264 KB)

MZH29 Chemical Structure

CAS No.: 2089590-80-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

MZH29 (1 mg/kg, p.o.) causes complete tumor regression and extends survival in a mouse model of AML with less toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2089590-80-5
Molecular Weight 560.62
Formula C₃₁H₃₃FN₄O₅
SMILES

O=C(NC1=CC=CC(C)=C1)NC2=CC=C(OC3=CC=NC4=CC(OCCCN5CCOCC5)=C(OC)C=C34)C(F)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Animals and Diseases

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (264 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xu B, et al. MZH29 is a novel potent inhibitor that overcomes drug resistance FLT3 mutations in acute myeloid leukemia. Leukemia. 2017 Apr;31(4):913-921. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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