1. Apoptosis
  2. MDM-2/p53

ALRN-6924 

Cat. No.: HY-112283
Handling Instructions

ALRN-6924 is a stapled peptide that blocks interactions between p53 and both MDM2 and MDMX. ALRN-6924 induces a complete remission in angioimmunoblastic T-cell lymphoma (AITL).

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

ALRN-6924 Chemical Structure

ALRN-6924 Chemical Structure

CAS No. : 2000293-14-9

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  • Biological Activity

  • Technical Information

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  • References

Description

ALRN-6924 is a stapled peptide that blocks interactions between p53 and both MDM2 and MDMX. ALRN-6924 induces a complete remission in angioimmunoblastic T-cell lymphoma (AITL)[1].

IC50 & Target

p53/MDM-2, p53/MDMX[1]

In Vitro

ALRN-6924 (0.01-10 μM; 72 hours) is potently active against all 9 TP53-wild-type cell lines (IC50 100 nM-4 μM) and in MTA cells, which harbor a heterozygous S215G mutation that is believed to confer loss-of-function[1].
In TP53-wild-type lines, ALRN-6924 (1.25-10 μM; 24 hours) induces a dose-dependent increase in levels of both p53 protein and the p53-target p21, which is associated with G0/G1 cell cycle arrest and induction of apoptosis[1].

Cell Cytotoxicity Assay[1]

Cell Line: MTA cells
Concentration: 0.01, 0.1, 1, and 10 μM
Incubation Time: 72 hours
Result: Potently active in MTA cells with IC50 of 100 nM-4 μM.

Western Blot Analysis[1]

Cell Line: TP53 wt (KI-JK, SUPM2, FEPD) and TP53 mutated (Karpas299) cell lines
Concentration: 1.25, 2.5, 5, and 10 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent increase in levels of both p53 protein and the p53-target p21 in TP53-wild-type lines, which was associated with G0/G1 cell cycle arrest and induction of apoptosis.
In Vivo

ALRN-6924 (20 mg/kg; given intravenously on days 1, 4, and 7) treatment induces p21 expression by IHC and apoptosis in treated tumors in mice. ALRN-6924 is broadly active across bone marrow, spleen and other involved compartments in all 8 models[1].

Animal Model: Mice with patient-derived xenograft (PDX) models WCTL-91953, DFTL-28776, and WCTL-81162[1]
Dosage: 20 mg/kg
Administration: Given intravenously on days 1, 4, and 7
Result: Treatment induced p21 expression by IHC and apoptosis in treated tumors.
References
CAS No.

2000293-14-9

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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ALRN-6924
Cat. No.:
HY-112283
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ALRN-6924

Cat. No.: HY-112283