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BA166663
BIO-X

APTO 253

Induces Kruppel like factor 4 (KLF4) and reduces the expression of MYC.  Anti-tumor activity of APTO 253 has been demonstrated in AML and haematological malignancies. Inducing KLP4 expression in ovarian cancer cells using APT0 253 sensitises cells to cisplatin  and paclitaxel. BRCA1/2-deficient cancer cells are hypersensitive to APTO 253, which mediates its action by causing DNA damage.

Technical Data

CAS No: 916151-99-0
Synonyms: LOR 253; 2-(5-Fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline
Product Code: BA166663
MDL No: MFCD25976826
Chemical Formula: C22H14FN5
Molecular Weight: 367.38

References


  • Kurtz ES et al (2015). Broad Activity of Apto-253 in AML and Other Hematologic Malignancies Correlates with KLF4 Expression Level. Blood 126(23):1358.
  • Wang B et al (2017). KLF4 expression enhances the efficacy of chemotherapy drugs in ovarian cancer cells. Biochem Biophys Res Commun 484(3):486-492.
  • Local A et al (2018). APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells 17(6):1177-1186.
  • Tsai CY et al (2018). APTO-253 Is a New Addition to the Repertoire of Drugs that Can Exploit DNA BRCA1/2 Deficiency. Mol Cancer Ther 17(6):1167-1176.

Solubility

Stability

Further Information


Datasheets

Specification: View
MSDS: View

APTO 253 - Bio-X

CAS No:
916151-99-0
Synonyms:
LOR 253
2-(5-Fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline
MDL No:
MFCD25976826
Chemical Formula:
Molecular Weight:
367.38
Product Structure
References:
1. Kurtz ES et al (2015). Broad Activity of Apto-253 in AML and Other Hematologic Malignancies Correlates with KLF4 Expression Level. Blood 126(23):1358.
2. Wang B et al (2017). KLF4 expression enhances the efficacy of chemotherapy drugs in ovarian cancer cells. Biochem Biophys Res Commun 484(3):486-492.
3. Local A et al (2018). APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells 17(6):1177-1186.
4. Tsai CY et al (2018). APTO-253 Is a New Addition to the Repertoire of Drugs that Can Exploit DNA BRCA1/2 Deficiency. Mol Cancer Ther 17(6):1167-1176.
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