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Development Status

Investigational

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Primary Target

Mitogen-activated protein kinase 11

2

Mitogen-activated protein kinase 12

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Mitogen-activated protein kinase 13

2

Mitogen-activated protein kinase 14

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cAMP-dependent protein kinase (PKA)

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Highest Phase

Phase II

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Approval Year

Unknown

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Condition

Colorectal cancer

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Metastatic colorectal cancer

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Multiple myeloma

2

Plasma cell neoplasm

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Recurrent or refractory multiple myeloma

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Treatment Modality

Primary

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Originator

Robins, R.K.|Revankar, G.R.|Chang, Y.

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Chemical

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CAS

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PUBCHEM

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ChEMBL

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DRUG BANK

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Salts, Hydrates, Esters, etc.

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8-Chloro-ATP

Z846LF5DED

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

p38 MAPK pathway

Mitogen-activated protein kinase 13

cAMP-dependent protein kinase (PKA)

Mitogen-activated protein kinase 12

Mitogen-activated protein kinase 14

Mitogen-activated protein kinase 11

Conditions:

Metastatic colorectal cancer

Recurrent or refractory multiple myeloma

Colorectal cancer

Multiple myeloma

Plasma cell neoplasm

8-Chloroadenosine-3',5'-cyclic-monophosphate (8-Cl-cAMP), an analog of c-AMP, is a novel antineoplastic agent. It has been shown to be effective against different human cancer cell lines modulating the cellular signal transduction pathway, thereby ca...

using growth inhibition, cell differentiation, and apoptosis. 8-Cl-cAMP preferentially binds to the R2 subunit of protein kinase A (PKA) and induces rapid R2 up-regulation and eventual R1 subunit down-regulation. It has potent inhibitory effects on a wide variety of human cancer cell lines, with an IC50 ranging from 0.1 to 20 uM. The IC50 falls with the length of drug exposure. It can suppress c-myc and c-ras proto-oncogenes in vitro and in vivo. It was shown that 8-Cl-cAMP induces cell growth inhibition through AMP-activated protein kinase (AMPK) activation with p38 MAPK acting downstream of AMPK in this signaling pathway. 8-Cl-cAMP induced apoptosis, apparently through activation of the p38 MAPK pathway by inducing progressive phosphorylation of the p38 mitogen-activated protein kinase (MAPK), via activation of AMPK by its metabolite 8-Cl-adenosine. 8-Cl-cAMP does not significantly inhibit the growth of NIH 3T3 cells, rat kidney fibroblasts, mammary epithelial cells, or peripheral blood lymphocytes, nor does it inhibit the growth of parental cells whose progeny have been transformed. Such selectivity makes it an attractive candidate for cancer therapy suggesting that it should not cause the toxicity of conventional cytotoxic agents but should inhibit tumor growth. 8-Cl-cAMP has been evaluated in phase I/II clinical trials.

TOCLADESINE

BQ94Z7E5OR

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Search for Structure

Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

p38 MAPK pathway

Mitogen-activated protein kinase 13

cAMP-dependent protein kinase (PKA)

Mitogen-activated protein kinase 12

Mitogen-activated protein kinase 14

Mitogen-activated protein kinase 11

Conditions:

Metastatic colorectal cancer

Recurrent or refractory multiple myeloma

Colorectal cancer

Multiple myeloma

Plasma cell neoplasm

8-Chloroadenosine-3',5'-cyclic-monophosphate (8-Cl-cAMP), an analog of c-AMP, is a novel antineoplastic agent. It has been shown to be effective against different human cancer cell lines modulating the cellular signal transduction pathway, thereby ca...

using growth inhibition, cell differentiation, and apoptosis. 8-Cl-cAMP preferentially binds to the R2 subunit of protein kinase A (PKA) and induces rapid R2 up-regulation and eventual R1 subunit down-regulation. It has potent inhibitory effects on a wide variety of human cancer cell lines, with an IC50 ranging from 0.1 to 20 uM. The IC50 falls with the length of drug exposure. It can suppress c-myc and c-ras proto-oncogenes in vitro and in vivo. It was shown that 8-Cl-cAMP induces cell growth inhibition through AMP-activated protein kinase (AMPK) activation with p38 MAPK acting downstream of AMPK in this signaling pathway. 8-Cl-cAMP induced apoptosis, apparently through activation of the p38 MAPK pathway by inducing progressive phosphorylation of the p38 mitogen-activated protein kinase (MAPK), via activation of AMPK by its metabolite 8-Cl-adenosine. 8-Cl-cAMP does not significantly inhibit the growth of NIH 3T3 cells, rat kidney fibroblasts, mammary epithelial cells, or peripheral blood lymphocytes, nor does it inhibit the growth of parental cells whose progeny have been transformed. Such selectivity makes it an attractive candidate for cancer therapy suggesting that it should not cause the toxicity of conventional cytotoxic agents but should inhibit tumor growth. 8-Cl-cAMP has been evaluated in phase I/II clinical trials.

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