China (Mainland)
Ceralasertib (AZD6738) CAS NO.1352226-88-0
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- Product Details
Keywords
- Ceralasertib
- AZD6738
- 1352226-88-0
Quick Details
- ProName: Ceralasertib (AZD6738)
- CasNo: 1352226-88-0
- Molecular Formula: C20H24N6O2S
- ProductionCapacity: Metric Ton/Day
- Purity: >97%
- LimitNum: 0 Metric Ton
Superiority
Biological Activity
| Description | Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. | ||||||||||||||||||||||||||||||
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| In vitro |
In four Kras mutant cell lines: H23, H460, A549, and H358, AZD6738 inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, AZD6738 strongly synergizes with cisplatin to induce rapid cell death. [1] In p53 or ATM defective cells, AZD6738 treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe. [2] |
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| Cell Data |
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| Assay |
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| In vivo | In nude mice bearing H460 and H23 tumors, AZD6738 (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and the the combination with cisplatin causes rapid regression of ATM-deficient H23 tumors. [1] In nude mice bearing LoVo xenografts, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. [3] |