1. MAPK/ERK Pathway
    Cell Cycle/DNA Damage
  2. KLF
    G-quadruplex

APTO-253 (Synonyms: LOR-253; LT-253)

Cat. No.: HY-16291 Purity: 96.80%
Handling Instructions

APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity.

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

APTO-253 Chemical Structure

APTO-253 Chemical Structure

CAS No. : 916151-99-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 456 In-stock
Estimated Time of Arrival: December 31
100 mg USD 696 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • References

Description

APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity.

IC50 & Target

KLF4[1], Gquadruplex[3]

In Vitro

APTO-253 is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by cisplatin 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (90.72 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 1.

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

    Solubility: 3.03 mg/mL (8.25 mM); Suspended solution; Need ultrasonic and warming

  • 2.

    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

References
Cell Assay
[3]

Cells are plated and treated with vehicle DMSO or APTO-253 (10 concentrations) in 96 well plates for 5 days at 37°C and 5% CO2. Cell viability is measured using CellTiter 96® AQueous one solution cell proliferation assay, and IC50 values are calculated using GraphPad Prism 7 software[3].

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

References
Molecular Weight

367.38

Formula

C₂₂H₁₄FN₅

CAS No.

916151-99-0

SMILES

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

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

Room temperature in continental US; may vary elsewhere

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Product Name:
APTO-253
Cat. No.:
HY-16291
Quantity:

APTO-253

Cat. No.: HY-16291