3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
- CAS NO.:860352-01-8
- Empirical Formula: C17H19FN4O2S
- Molecular Weight: 362.42
- MDL number: MFCD12406007
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-07 08:52:35
What is 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide?
Description
Actively proliferating cells experience blocks at certain checkpoints in the cell cycle when DNA damage is detected. These checkpoints allow for DNA damage repair before further cell cycle progression. Targeting signaling pathways to selectively inhibit repair at these checkpoints in tumor cells is of considerable interest to cancer therapeutics. AZD 7762 selectively inhibits the activity of checkpoint kinases (Chk) 1 and Chk2 (IC50s = 5 nM) by competitively and reversibly binding their respective ATP-
The Uses of 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
AZD 7762 is studied as an cancer therapeutic agent due to its selective inhibitory activities towards checkpoint kinases, chk1 and chk2 by reversibly binding their respective ATP-binding sites within tumor cells. Recent research has also indicated AZD 7762 to possess enhancing effects towards other chk1 inhibitor lethality in glioblastoma cells.
What are the applications of Application
AZD7762 is a checkpoint kinase inhibitor for Chk1 and Chk2
Definition
ChEBI: 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-3-piperidinyl]-2-thiophenecarboxamide is an aromatic amide and a member of thiophenes.
References
1) Zabludoff?et al.?(2008)?AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies; Mol. Cancer Ther.?7?2955 2) Mitchell?et al.?(2010)?In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762; Clin. Cancer Res.?16?2076 3) Morgan?et al. (2010)?Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair; Cancer Res.?70?49721 4) Lei?et al.?(2018)?Chk1 inhibitors overcome imatinib resistance in chronic myeloid leukemia cells; Leuk. Res.?64?17 5) Ahmad?et al. (2015)?Identification of Ponatinib and Other Known Kinase Inhibitors with Potent MEKK2 Inhibitory Activity;?Biochem. Biophys. Res. Commun.?463?888 6) Park?et al.?(2018)?Repositioning of anti-cancer drug candidate, AZD7762, to an anti-allergic drug suppressing IgE-mediated mast cells and allergic responses via the inhibition of Lyn and Fyn; Biochem. Pharmacol.?154?270
Properties of 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
Boiling point: | 547.6±50.0 °C(Predicted) |
Density | 1.38 |
storage temp. | -20° |
solubility | Soluble in DMSO (up to at least 25 mg/ml). |
form | solid |
pka | 9.06±0.20(Predicted) |
color | Yellow or brown |
Stability: | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
Safety information for 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
Computed Descriptors for 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-Thiophenecarboxamide
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