PROTAC FLT-3 degrader 3
PROTAC FLT-3 degrader 3 is a FLT-3 PROTAC degrader. PROTAC FLT-3 degrader 3 reduces the phosphorylation levels of FLT3-ITD, AKT, STAT5 and ERK. PROTAC FLT-3 degrader 3 induces apoptosis and cell cycle arrest in leukemia cells. PROTAC FLT-3 degrader 3 can be used for the research of acute myeloid leukemia.
(Pink: FLT3 ligand (HY-175900); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Formula: C48H44Cl2N10O6
- Molecular Weight:927.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10000 nM
Compound: 35
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Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| LoVo | IC50 |
>10000 nM
Compound: 35
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Antiproliferative activity against human LoVo cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human LoVo cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| MDA-MB-231 | IC50 |
6482 nM
Compound: 35
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| MOLM-13 | IC50 |
18.23 nM
Compound: 35
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Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| MV4-11 | IC50 |
7.55 nM
Compound: 35
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Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD mutant assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD mutant assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| NCI-N87 | IC50 |
>10000 nM
Compound: 35
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Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| Panc02 | IC50 |
>10000 nM
Compound: 35
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Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against mouse Panc02 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| U-937 | IC50 |
>10000 nM
Compound: 35
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Antiproliferative activity against human U-937 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human U-937 cells assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
|
[PMID: 38387337] |
PROTAC FLT-3 degrader 3 (Compound 35) (72 h) potently inhibits the proliferation of MV4-11 acute myeloid leukemia cells, with an IC50 of 7.55 nM[1].
PROTAC FLT-3 degrader 3 (72 h) selectively inhibits the proliferation of FLT3-mutant leukemia cell lines (MOLM13, HCD57-FLT3-ITD, HCD57-FLT3-D835H) with IC50 values of 18.23, 11.75, and 11.19 nM, respectively. It exhibits only weak activity against MDA-MB-231 cells (IC50 = 6482 nM) and no activity against HCD57, U937, NCI-N87, LOVO, A549, and Panc 02 cells[1].
PROTAC FLT-3 degrader 3 (0.1-100 nM) dose-dependently degrades FLT3-ITD and reduces the phosphorylation levels of FLT3-ITD, AKT, STAT5 and ERK in MV4-11 cells[1].
PROTAC FLT-3 degrader 3 (0-500 nM) induces apoptosis in MV4-11 cells in a dose-dependent manner[1].
PROTAC FLT-3 degrader 3 (0-100 nM) dose-dependently arrests MV4-11 cells at the G1 phase of the cell cycle[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 927.83
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Formula C48H44Cl2N10O6
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SMILES
O=C1C(CCC(N1)=O)N(C2=O)C(C3=C2C(N4CCN(C(CC5CCN(C6=CC=C(C(NC7=NNC(C8=CC(N(CC9=C(Cl)C=CC=C9Cl)C=N%10)=C%10C=C8)=C7)=O)C=C6)CC5)=O)CC4)=CC=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC FLT-3 degrader 3 Related Classifications
HY-161280 Related Classifications
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