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Myc proto-oncogene protein

2

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

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Lorus Therapeutics

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APTO-253

WB59MRW00U

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Myc proto-oncogene protein

Krueppel-like factor 4

Conditions:

Non-small cell lung cancer

Haematological malignancies

Myelodysplastic syndromes

APTO-253 is a novel small molecule that can induce expression of the genes that code for the Krüppel-like factor 4 (KLF4) master transcription factor and for the p21 cell cycle inhibitor protein, and can inhibit expression of the c-Myc oncogene, lead...

ing to cell cycle arrest and programmed cell death (apoptosis) in human-derived solid tumor and hematologic cancer cells. A Phase 1 study with APTO-253 was completed and demonstrated modest clinical activity in patients with colon cancer, acute leukemia, myelodysplastic syndrome, hematological malignancies and non-small cell lung cancers.

APTO-253 HYDROCHLORIDE

266N56YWTZ

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Myc proto-oncogene protein

Krueppel-like factor 4

Conditions:

Non-small cell lung cancer

Haematological malignancies

Myelodysplastic syndromes

APTO-253 is a novel small molecule that can induce expression of the genes that code for the Krüppel-like factor 4 (KLF4) master transcription factor and for the p21 cell cycle inhibitor protein, and can inhibit expression of the c-Myc oncogene, lead...

ing to cell cycle arrest and programmed cell death (apoptosis) in human-derived solid tumor and hematologic cancer cells. A Phase 1 study with APTO-253 was completed and demonstrated modest clinical activity in patients with colon cancer, acute leukemia, myelodysplastic syndrome, hematological malignancies and non-small cell lung cancers.

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