product name AZD6738
Description: AZD6738 is an orally available morpholino-pyrimidine-based, and selective ATR kinase inhibitor with IC50 of 1 nM. AZD6738 has potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis.
References: Lancet. 2015 Feb 26;385 Suppl 1:S58; Sci Rep. 2015 Aug 27;5:13545.
412.51
Formula
C20H24N6O2S
CAS No.
1352226-88-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 82 mg/mL (198.7 mM)
Water: <1 mg/mL
Ethanol: 41 mg/mL warmed (99.4 mM)
Solubility (In vivo)
10% DMSO+40% propylene glycol+ddH2O: 10mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19395434
| In Vitro |
In vitro activity: In an in vitro model capable of reproducing, over 70 hours after the initiation of the treatment with AZD6738, the γH2AX signal was sustained. Stalled replication forks may collapse the formation of DNA double stranded breaks and the activation of the ataxia telangiectasia mutated (ATM) kinase. As a single agent across cancer cell line panels, AZD6738 is active. In cell lines lacking ATM-pathway, the sensitivity of AZD6738 was enhanced. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In ATM-deficient but not ATM-proficient in vivo models, treatment with AZD6738 alone significantly inhibited the activity of tumors in equivalent, tolerated doses. Ionizing radiation (IR) is a DNA damaging inducing agent. When AZD6738 and IR were used together, regression or anti-tumor growth inhibitory activity was observed. In tumor tissue, AZD6738 is associated with a persistent γH2AX staining increase. In normal gut tissue or bone marrow, treatment with AZD6738 only transiently increased the γH2AX staining. |
| Animal model | |
| Formulation & Dosage | |
| References | Lancet. 2015 Feb 26;385 Suppl 1:S58; Sci Rep. 2015 Aug 27;5:13545. |
Related Posts
product name AZD6738
Description: AZD6738 is an orally available morpholino-pyrimidine-based, and selective ATR kinase inhibitor with IC50 of 1 nM. AZD6738 has potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor AZD6738 selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis.
References: Lancet. 2015 Feb 26;385 Suppl 1:S58; Sci Rep. 2015 Aug 27;5:13545.
412.51
Formula
C20H24N6O2S
CAS No.
1352226-88-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 82 mg/mL (198.7 mM)
Water: <1 mg/mL
Ethanol: 41 mg/mL warmed (99.4 mM)
Solubility (In vivo)
10% DMSO+40% propylene glycol+ddH2O: 10mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19395434
| In Vitro |
In vitro activity: In an in vitro model capable of reproducing, over 70 hours after the initiation of the treatment with AZD6738, the γH2AX signal was sustained. Stalled replication forks may collapse the formation of DNA double stranded breaks and the activation of the ataxia telangiectasia mutated (ATM) kinase. As a single agent across cancer cell line panels, AZD6738 is active. In cell lines lacking ATM-pathway, the sensitivity of AZD6738 was enhanced. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In ATM-deficient but not ATM-proficient in vivo models, treatment with AZD6738 alone significantly inhibited the activity of tumors in equivalent, tolerated doses. Ionizing radiation (IR) is a DNA damaging inducing agent. When AZD6738 and IR were used together, regression or anti-tumor growth inhibitory activity was observed. In tumor tissue, AZD6738 is associated with a persistent γH2AX staining increase. In normal gut tissue or bone marrow, treatment with AZD6738 only transiently increased the γH2AX staining. |
| Animal model | |
| Formulation & Dosage | |
| References | Lancet. 2015 Feb 26;385 Suppl 1:S58; Sci Rep. 2015 Aug 27;5:13545. |