[CAS NO. 916151-99-0] APTO-253

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PRODUCTS SPECIFICATIONS [916151-99-0]

Catalog

HY-16291

Brand

MCE

CAS

916151-99-0

DESCRIPTION [916151-99-0]

Overview

MDL	MFCD25976826
Molecular Weight	367.38
Molecular Formula	C22H14FN5
SMILES	CC(N1)=C(C(N2)=NC3=C2C4=CC=CN=C4C5=NC=CC=C53)C6=C1C=CC(F)=C6

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

8 Publications Citing Use of MCE

Summary

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 ^[1] ^[2] . APTO-253 has antiarthritic activity ^[3] .

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 IC ₅₀ s 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 IC ₅₀ s 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] .

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] .

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
NCT02267863	Aptose Biosciences Inc.	Acute Myelogenous Leukemia in Relapse\|Acute Myelogenous Leukemia, Relapsed, Adult\|Acute Myelogenous Leukemia, Adult\|Acute Myelogenous Leukemia\|High Risk Myelodysplasia	October 2014	Phase 1
NCT01281592	Aptose Biosciences Inc.	Advanced or Metastatic Solid Tumours	January 2011	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 60 mg/mL ( 163.32 mM ; Need ultrasonic)

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 >> 40% PEG300 >> 5% Tween-80 >> 45% saline

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

* All of the co-solvents are available by MCE.