Art. -Nr.: HY-16291

APTO-253

(Synonyms: LOR-253; LT-253)

21 Cited Publications

Kundenbewertung

Based on 21 publication(s) in Google Scholar

APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity.

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Reinheit: 99.74%
CAS. Nr.: 916151-99-0
Formel: C₂₂H₁₄FN₅
Molecular Weight:367.38

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

APTO-253 Chemical Structure

CAS. Nr.: 916151-99-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (21)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

c-Myc^[1]; KLF4^[2]

In Vitro

APTO-253 (LOR-253) is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by NSC 119875 in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells^[1].
APTO-253 is cytotoxic to Raji and Raji/253R cell lines, with IC₅₀s of 105 ± 2.4 nM and 1387 ± 94 nM, respectively. APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R^[2].
APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines with IC₅₀s ranging from 57 nM to 1.75 μM. APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down regulates MYC RNA and protein expression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells. Futhermore, APTO-253 is a potent stabilizer of Gquadruplex (G4) motifs, and demonstrates the greatest propensity for stabilizing the MYC G4 sequences^[3].

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

In Vivo

APTO-253 (LOR-253; 15 mg/kg; IV; twice per day for 2 consecutive days per week for 14 days) has antiarthritic activity in a CIA model^[3].

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

Animal Model:

DBA/1J male mice (6 weeks) with collagen induced arthritis (CIA)^[3]
Dosage:

15 mg/kg
Administration:

IV; twice per day for 2 consecutive days per week for 14 days
Result:

Demonstrated significant preventive and therapeutic activity on arthritis formation.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 916151-99-0
Appearance Solid
Molecular Weight 367.38
Formel C₂₂H₁₄FN₅
Color Light yellow to yellow
SMILES

CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6
Synonyms

LOR-253; LT-253
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (21)

All Cell Proliferation/Viability AssayRT-PCRWBIn Vivo Efficacy Study

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Journal Impact Factor

Ann Rheum Dis

Parsing multiomics landscape of activated synovial fibroblasts highlights drug targets linked to genetic risk of rheumatoid arthritis. [Abstract]

2021 Apr;80(4):440-450. PMID: 33139312

APTO-253 purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2021 Apr;80(4):440-450. [Abstract]

APTO-253 (1-4 μM) reduced mRNA levels of 8-mix SE-contacted genes (IL-6, CCL5) in stimulated RASFs.

APTO-253 purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2021 Apr;80(4):440-450. [Abstract]

APTO-253 (15 mg/kg; i.v.; twice per day for two consecutive days per week) demonstrated significant therapeutic activity in collagen-induced arthritis (CIA) mice.
Blood

Epigenetic Regulation of Non-canonical Menin Targets Modulates Menin Inhibitor Response in Acute Myeloid Leukemia. [Abstract]

2024 Aug 16:blood.2023023644. PMID: 39158067

APTO-253 purchased from MedChemExpress. Usage Cited in: Blood. 2024 Aug 16:blood.2023023644. [Abstract]

Cell viability of OCI-AML2 cells expressing either sgLuc or sgPCGF1 was assessed under the treatment of APTO-253 (100 nM; 9 d).
Nat Commun

FAM3A reshapes VSMC fate specification in abdominal aortic aneurysm by regulating KLF4 ubiquitination. [Abstract]

2023 Sep 2;14(1):5360. PMID: 37660071

APTO-253 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 2;14(1):5360. [Abstract]

APTO-253 (10 μM) reversed the effects of FAM3A on suppressing the expression of the markers for macrophages (CD68) and osteoblasts (OPN, RUNX2) in VSMCs.

APTO-253 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 2;14(1):5360. [Abstract]

KLF4 inducer APTO-253 (1 μg/g; i.p.; once daily for 4 weeks) significantly abrogated the effects of FAM3A on maintaining the contractile phenotype of VSMCs in aortas from AngII-ApoE^−/− murine AAA models.
Nat Commun

Chromatin-informed inference of transcriptional programs in gynecologic and basal breast cancers. [Abstract]

2019 Sep 25;10(1):4369. PMID: 31554806
Adv Sci (Weinh)

Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization. [Abstract]

2025 Mar 24:e2408992. PMID: 40126336
J Transl Med

KLF4 regulates trophoblast function and associates with unexplained recurrent spontaneous abortion. [Abstract]

2024 Oct 10;22(1):922. PMID: 39390495
Leukemia

Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]

2025 Sep;39(9):2163-2173. PMID: 40670672
Cell Rep

SETDB2-mediated transcriptional repression of IDE in sensory neurons promotes migraine-like pain behaviors in mice. [Abstract]

2026 Mar 24;45(4):117201. PMID: 41880325
JCI Insight

KLF4 is a therapeutically tractable brake on fibroblast activation that promotes resolution of pulmonary fibrosis. [Abstract]

2022 Aug 22;7(16):e160688. PMID: 35852857
J Environ Sci

2025 Nov 28.
Int Immunopharmacol

Succinate pretreatment attenuates intestinal ischemia-reperfusion injury by inhibiting necroptosis and inflammation via upregulating Klf4. [Abstract]

2023 Jul:120:110425. PMID: 37285681
PLoS Pathog

STAT3, MYC, and EBNA1 cooperate through a ZC3H18 transcriptional network to regulate survival and proliferation of EBV-positive lymphomas. [Abstract]

2025 May 12;21(5):e1013166. PMID: 40354417
Mol Cell Biochem

Expressions and related mechanisms of miR-212 and KLF4 in rats with acute kidney injury. [Abstract]

2021 Apr;476(4):1741-1749. PMID: 33428060
FASEB J

Induction of T-Cell Differentiation by KLF4 in T-Cell Acute Lymphoblastic Leukemia Cells Harboring Activating Mutation in NOTCH3. [Abstract]

2025 May 31;39(10):e70613. PMID: 40354086
J Immunol

TLR7-mediated immune response of renal myeloid-derived suppressor cells via RUNX1-KLF4 in systemic candidiasis. [Abstract]

2025 Aug 7:vkaf170. PMID: 40795213
Neurotox Res

The MT1G Gene in LUHMES Neurons Is a Sensitive Biomarker of Neurotoxicity. [Abstract]

2020 Dec;38(4):967-978. PMID: 32870474
J Diabetes Res

KLF4 Promotes Diabetic Chronic Wound Healing by Suppressing Th17 Cell Differentiation in an MDSC-Dependent Manner. [Abstract]

2021 Sep 15:2021:7945117. PMID: 34568499
Genes (Basel)

Krüppel-Like Factor 4 and Its Activator APTO-253 Induce NOXA-Mediated, p53-Independent Apoptosis in Triple-Negative Breast Cancer Cells. [Abstract]

2021 Apr 8;12(4):539. PMID: 33918002
Research Square Preprint

2023 Jun 29.
Research Square Preprint

2023 Apr 18.
Patent

US20220332841A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (68.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7220 mL

13.6099 mL

27.2198 mL

5 mM

0.5444 mL

2.7220 mL

5.4440 mL

10 mM

0.2722 mL

1.3610 mL

2.7220 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.3 mg/mL (6.26 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (23.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (5.66 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (27.22 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC-Na/0.1% Tween-80 in Saline water

Solubility: 5 mg/mL (13.61 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)

Verweise

[1]. Local A, et al. APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells. Mol Cancer Ther. 2018 Jun;17(6):1177-1186. [Content Brief]

[2]. Hongying Zhang, et al. Inhibition of c-Myc By Apto-253 As an Innovative Therapeutic Approach to Induce Cell Cycle Arrest and Apoptosis in Acute Myeloid Leukemia. Blood 2016 128:1716.

[3]. Haruka Tsuchiya, et al. Parsing multiomics landscape of activated synovial fibroblasts highlights drug targets linked to genetic risk of rheumatoid arthritis. Ann Rheum Dis. 2020 Nov2;annrheumdis-2020-218189. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7220 mL	13.6099 mL	27.2198 mL	68.0494 mL
	5 mM	0.5444 mL	2.7220 mL	5.4440 mL	13.6099 mL
	10 mM	0.2722 mL	1.3610 mL	2.7220 mL	6.8049 mL
	15 mM	0.1815 mL	0.9073 mL	1.8147 mL	4.5366 mL
	20 mM	0.1361 mL	0.6805 mL	1.3610 mL	3.4025 mL
	25 mM	0.1089 mL	0.5444 mL	1.0888 mL	2.7220 mL
	30 mM	0.0907 mL	0.4537 mL	0.9073 mL	2.2683 mL
	40 mM	0.0680 mL	0.3402 mL	0.6805 mL	1.7012 mL
	50 mM	0.0544 mL	0.2722 mL	0.5444 mL	1.3610 mL
	60 mM	0.0454 mL	0.2268 mL	0.4537 mL	1.1342 mL

Keywords

APTO-253

21 Cited Publications

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APTO-253

Apoptosis Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) APTO-253

Biologische Aktivität

Chemical Information

Publications (21)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APTO-253

Apoptosis Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Mitochondrial Protection Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) APTO-253

Biologische Aktivität

Chemical Information

Publications (21)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APTO-253 Related Classifications

HY-16291 Related Classifications