计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存,干燥。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC 50 s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC 50 s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity
In Vitro
GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells. GZD856 (0.3-3 μM; 24-28 h) induces a dose-dependent G0/G1 phase arrest and apoptosis in H1703 but not A549 cells. GZD856 (0.1-10 μM; 6 h) dose-dependently inhibits the PDGFRα/β phosphorylation and downstream signaling in H1703 and A549 cells. GZD856 inhibits the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-Abl WT and Bcr-Abl T315I , with IC 50 s of 2.2, 67.0, 0.64 and 10.8 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: H1703, A549, Calu-6, 95-D, L-78, HCC827, SPCA-1, H1650, H1299, H522, H332 and H820 NSCLC cells Concentration: 0.0032-10 μM Incubation Time: 72 hours Result: Inhibited PDGFRα-overexpressing H1703 cells, with an IC 50 of 0.25 μM. Apoptosis AnalysisCell Line: H1703 and A549 NSCLC cells Concentration: 0.3, 1, 3 μM Incubation Time: 24, 48 hours Result: Led to 54.1% apoptosis in H1703 cells at the concentration of 3.0 µM, whereas only 15.5% apoptotic A549 cells were observed under similar conditions. Decreased the CDK4, cyclin D2, CDK2 and Cyclin E protein levels and activated of PARP and Caspase-3 cleavage in H1703 cells. Western Blot AnalysisCell Line: H1703 and A549 NSCLC cells Concentration: 0.1-10 μM Incubation Time: 6 hours Result: Inhibited the phosphorylation of PDGFRα and PDGFRβ in a dose-dependent manner. Observed the activation of downstream AKT, ERK1/2 and STAT3, with no obvious effects on total protein levels.
In Vivo
GZD856 (10-30 mg/kg, p.o. once daily for 16 d) displays good antitumor activity in both H1703 and A549 lung cancer models and is well tolerated. GZD856 inhibits brain and liver metastasis of lung cancer cells in an A549-Luc orthotopic model . GZD856 (10 mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-Abl T315I. GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T 1/2 =19.97 h), optimal plasma exposure (C max =934.38 μg/L) and a AUC 0-∞ (8165.8 µg/L•h) in rats . GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T 1/2 =22.2 h), optimal plasma exposure (C max =899.5 μg/L) and a good oral bioavailability (BA=78%) in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CB17-SCID mice implanted with H1703 and A549 cancer cells Dosage: 10, 30 mg/kg Administration: Oral gavage once daily for 16 days Result: Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively. Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg. Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight. Animal Model: Sprague-Dawley (SD) rats (180-220 g) Dosage: 5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis) Administration: A single intravenous injection and oral administration Result: I.v.: T 1/2 =19.97 h; C max =934.38 μg/L; AUC 0-∞ =8165.8 µg/L•h. P.o.: T 1/2 =22.2 h; C max =899.5 μg/L; BA=78%.
Form:Solid
IC50& Target:PDGFRα|68.6 nM (IC|50|)|PDGFRβ|136.6 nM (IC|50|)|Bcr-Abl|T315I|15.4 nM (IC|50|)|Bcr-Abl|19.9 nM (IC|50|)
规格
别名
GZD856 甲酸
规格或纯度
≥98%
英文名称
GZD856 formic
生化机理
GZD856 甲酸盐是一种强效的口服活性 PDGFRα/β 抑制剂，其 IC 50 s 分别为 68.6 和 136.6 nM。GZD856 甲酸盐也是一种 Bcr-Abl T315I 抑制剂，对原生 Bcr-Abl 和 T315I 突变体的 IC 50 s 分别为 19.9 和 15.4u2009nM。GZD856 甲酸盐
储存条件
-20°C储存,干燥
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
578.58
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (172.84 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2804039-78-7，分子式为 C30H29F3N6O3，分子量为 578.58 g/mol。
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每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
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