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- 2025年12月05日
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- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
405168-58-3
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1023.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥930.0 |
| 规格： | 10 mg | 产品价格： | ￥1581.0 |
| 规格： | 25 mg | 产品价格： | ￥3000.0 |
| 规格： | 50 mg | 产品价格： | ￥5580.0 |
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CHIR-124
CAS No. : 405168-58-3
MCE 国际站：CHIR-124
产品活性：CHIR-124 是一种有效的，选择性的 Chk1 抑制剂，IC50 值为 0.3 nM；同时可有效抑制 PDGFR 和 FLT3，IC50 值分别为 6.6 nM 和 5.8 nM。
研究领域：Cell Cycle/DNA Damage | Protein Tyrosine Kinase/RTK | Apoptosis
作用靶点：Checkpoint Kinase (Chk) | FLT3 | PDGFR | Apoptosis
In Vitro: CHIR-124 is 500- to 5,000-fold less active against other cell cycle kinases, such as cyclin-dependent kinase 2/cyclin A (0.19 μM), cdc2/cyclin B (0.51 μM), and cyclin-dependent kinase 4/cyclin D (2.1 μM). CHIR-124 (≥0.9 nM) in combination with SN-38 (≥0.42 nM) causes significant synergy or >10% deviation from additivity in human cancer cell lines expressing mutant p53, and these values overlap and fall below the IC50s for SN-38 (1.2×10-7 M) and CHIR-124 (2.2×10-7 M), respectively. Moreover, CHIR-124 (100 nM) abrogates the SN-38-induced S and G2-M phase cell cycle checkpoints. CHIR-124 (200 nM) leads to a 2.5-fold elevated level of cdc25A above that of the untreated HCT116 p53 / cells. The down-regulation of cdc25A induced by SN-38 is completely restored by concurrent or sequential treatment with CHIR-124, proving that CHIR-124 inhibits the Chk1-mediated destruction of cdc25A in whole cells. CHIR-124 occupies the ATP-binding site, inhibits Chk1 (IC50, 0.3 nM) 2,000-fold more potently than Chk2 (IC50, 0.7 μM).
In Vivo: CHIR-124 (10 or 20 mg/kg, p.o.) does not have a significant effect on tumor growth when compared with the vehicle-treated group, but it potentiates the growth inhibitory effect of CPT-11 in a human breast carcinoma xenograft model. The potentiation of the tumor growth inhibitory effect of CPT-11 by CHIR-124 is associated with an increase in apoptosis induction in the tumors. CHIR-124 reverses the suppression of phospho-H3 staining induced by CPT-11, indicating abrogation of the G2-M checkpoint by CHIR-124.
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文献和实验/100)；主要病毒为HBV 20.16%(25/124)，HCV 9.68%(12/124)，二者均高于非ALD组9%、2%与报道的本地区自然人群HBsAg和抗HCV阳性率11.12%、2.29%；其它各型肝炎病毒检出率与对照组无差异。PHC患者肝炎病毒检出率最高，为75%(9/2)，AC次之，为58.33%(14/24)，二者之和为63.89%(23/36)，显著高于非硬化组25%(22/88)，表明长期过量饮酒可增加HBV和HCV的易感性，且随着ALD的病程进展肝炎病毒的检出率逐步升高。本组
124 88 0.25 0.30 123 87 61 0.30 0.35 110 90 64 102 45 0.35 0.40 85 70 100 50 108 78 35 0.40 0.45 118 68 101 55 105 79 39 108 86 62
124 88 0.25 0.30 123 87 61 0.30 0.35 110 90 64 102 45 0.35 0.40 85 70 100 50 108 78 35 0.40 0.45 118 68 101 55 105 79 39 108 86 62
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