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| 产地 | 中国 |
| 品牌 | Chemstan |
| 货号 | LC-01 |
| 用途 | 中间体 |
| 包装规格 | 20mg |
| 纯度 | 98%% |
| CAS编号 | 860352-01-8 |
| 是否进口 | 否 |
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Fields of Application :
AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM; equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
| CAS Number: | 860352-01-8 |
| Purity: | >98% |
| Molecular Weight: | 398.889 |
| Molecular Formula: | C17H19FN4O2S.HCl |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | AZD7762; AZD-7762 |
| Chemical Name: | 1-(2-((S)-piperidin-3-ylcarbamoyl)-5-(3-fluorophenyl)thiophen-3-yl)urea |
| Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
AZD7762, a more selective Chk1 inhibitor, inhibits Chk1 phosphorylation of a cdc25C peptide by reversibly binding to the ATP-binding site of Chk1, with IC50 of 5 nM and Ki of 3.6 nM. AZD7762 induces cell arrest with EC50 of 0.620 μM, and significantly abrogates the camptothecin induced G2 arrest with an EC50 of 10 nM, by blocking the chk1 dependent degradation of Cdc25A and activation of Cyclin A. AZD7762 (300 nM) enhances the antitumor efficacy of gemcitabine against SW620 and topotecan against MDA-MB-231 by reducing the GI50 values from 24.1 nM and 2.25 μM to 1.08 nM and 0.15 μM, respectively. AZD7762 shows cytotoxicity against a variety of neuroblastoma cell lines bearing p53 wild type, p53 mutation, Mdm2 amplification or p14 deletion with IC50 values ranging from 82.6-505.9 nM. AZD7762 alone at 25 mg/kg shows little antitumor activity in the H460-DNp53 xenograft mice and SW620 xenograft mice, but when administrated in combination with gemcitabine (60 mg/kg), AZD7762 shows significant antitumor efficacy in the two xenografts mice with a log cell kill of 0.9 or percent treated/control (%T/C) of 26 even at low dose of 12.5 mg. Dosing of AZD7762 in combination with gemcitabine (10 mg/kg) in the H460-DNp53 xenograft rat inhibits the tumor volume in a dose-dependent manner with the %T/C values of 48 and 32 For 10 and 20 mg/kg AZD7762, respectively. AZD7762 (25 mg/kg) in combination with irinotecan (25 or 50 mg/kg) causes complete tumor regression in the SW620 xenograft mice with the %T/C increasing significantly to -66% and -67%, respectively. For the detailed information of AZD 7762, the solubility of AZD 7762 in water, the solubility of AZD 7762 in DMSO, the solubility of AZD 7762 in PBS buffer, the animal experiment (test) of AZD 7762, the cell expriment (test) of AZD 7762, the in vivo, in vitro and clinical trial test of AZD 7762, the EC50, IC50,and Affinity of AZD 7762.
References:
N(C1C=C(C2=CC=CC(F)=C2)SC=1C(=O)N[C@@H]1CCCNC1)C(N)=O
