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Referencia número: HY-162462

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Antitumor agent-151

Antitumor agent-151 (7k) is a significant HsClpP agonist and an antileukemia drug candidate. Antitumor agent-151 (7k) exhibits remarkably enhanced proteolytic activity of HsClpP (EC₅₀ = 0.79 μM) and antitumor activity in vitro (IC₅₀ = 0.038 μM). Antitumor agent-151 (7k) induces apoptosis.

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No. CAS: 3036751-77-3
Fòrmula: C₂₂H₂₀FN₅O
Peso molecular:389.43

Almacenamiento:

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

Data Sheet (265 KB)

Antitumor agent-151 Chemical Structure

No. CAS: 3036751-77-3

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Use of MCE Products

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

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	IC₅₀	>20 nM Compound: 7k	Cytotoxicity against normal bone marrow cell (unknown origin) assessed as cell proliferation incubated for 72 hrs by CCK-8 assay Cytotoxicity against normal bone marrow cell (unknown origin) assessed as cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
HL-60	IC₅₀	40.5 nM Compound: 7k	Anti-leukemia activity against human HL-60 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human HL-60 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
K562	IC₅₀	131.8 nM Compound: 7k	Anti-leukemia activity against human K562 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human K562 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
Kasumi 1	IC₅₀	41.1 nM Compound: 7k	Anti-leukemia activity against human Kasumi 1 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human Kasumi 1 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
MOLM-13	IC₅₀	30.1 nM Compound: 7k	Anti-leukemia activity against human MOLM-13 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human MOLM-13 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
MV4-11	EC₅₀	0.078 μM Compound: 7k	Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 48 hrs by CCK-8 assay Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 48 hrs by CCK-8 assay	[PMID: 38620134]
MV4-11	EC₅₀	5.2 μM Compound: 7k	Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 24 hrs by CCK-8 assay Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 24 hrs by CCK-8 assay	[PMID: 38620134]
MV4-11	IC₅₀	0.03 μM Compound: 7k	Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
OCI-AML2	IC₅₀	39.2 nM Compound: 7k	Anti-leukemia activity against human OCI-AML2 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human OCI-AML2 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
THP-1	IC₅₀	79.7 nM Compound: 7k	Anti-leukemia activity against human THP-1 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human THP-1 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]
U-937	IC₅₀	78.2 nM Compound: 7k	Anti-leukemia activity against human U-937 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay Anti-leukemia activity against human U-937 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 38620134]

In Vitro

Antitumor agent-151 (7k) displays a strong activity for inhibition of other AML cell lines. The IC₅₀ values of Molm13, U937, OCI-AML2, THP-1, HL60, KASSUMI, and K562 cell lines are 30.1 ± 2.3, 78.2 ± 3.1, 39.2 ± 0.9, 79.7 ± 0.3, 40.5 ± 0.8, 41.1 ± 1.7, and 131.8 ± 1.5 nM, respectively^[1].

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

In Vivo

Antitumor agent-151 (7k, 10 mg/kg, ip, Female BALB/c nude mice bearing Mv4-11 AML cells) shows powerful antitumor efficacy^[1].

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

Chemical Information

No. CAS 3036751-77-3
Peso molecular 389.43
Fòrmula C₂₂H₂₀FN₅O
SMILES

O=C(C1=C(CCN(C1)CC2=CC(C#N)=CC=C2)N3)N=C3NCC4=CC=C(C=C4)F
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (265 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Xinrong Xiang, et al. Rational Design of a Novel Class of Human ClpP Agonists through a Ring-Opening Strategy with Enhanced Antileukemia Activity. J Med Chem. 2024 Apr 25;67(8):6769-6792. [Content Brief]

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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.

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