1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. PAK

APTO-253 (Synonyms: LOR-253; LT-253)

Cat. No.: HY-16291 Purity: 99.16%
Data Sheet SDS Handling Instructions

APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $88 In-stock
5 mg $80 In-stock
10 mg $120 In-stock
50 mg $380 In-stock
100 mg $580 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

APTO-253 is a novel small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Krüppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death. Target: p21 in vitro: APTO-253 demonstrats potent and selective growth inhibition of a variety of solid tumor cell lines, including colon cancer, non-small cell lung cancer (NSCLC), prostate cancer and melanoma, with IC50 values of 0.04- 2.6 μM. APTO-253 demonstrats even great potency of growth inhibitory activity against leukemia cell lines, including AML, ALL and chronic myeloid leukemia (CML), as well as non-Hodgkin's lymphoma (NHL) cell lines, with IC50 values ranging from 7 nM - 0.3 μM.[1] in vivo: Nonclinical pharmacology studies have demonstrated that APTO-253 exerts in vivoanti-tumor activity in solid tumors and hematologic cancers. [1]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02267863 Aptose Biosciences Inc. Relapsed Hematologic Malignancies|Refractory Hematologic Malignancies October 2014 Phase 1
NCT02267863 Aptose Biosciences Inc. Relapsed Hematologic Malignancies|Refractory Hematologic Malignancies October 2014 Phase 1
NCT01281592 Aptose Biosciences Inc. Advanced or Metastatic Solid Tumours January 2011 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
References
M.Wt

367.38

Formula

C₂₂H₁₄FN₅

CAS No.

916151-99-0

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

Solvent & Solubility

DMSO: ≥ 26 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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