GNF-7|cas:839706-07-9|西域试剂

GNF-7,98.93%

产品编号：Bellancom-10943| CAS NO：839706-07-9| 分子式：C₂₈H₂₄F₃N₇O₂| 分子量：547.53

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10943	￥1080.00	杭州北京（现货）
Bellancom-10943	￥1800.00	杭州北京（现货）
Bellancom-10943	￥3500.00	杭州北京（现货）
Bellancom-10943	￥6000.00	杭州北京（现货）
Bellancom-10943	￥10500.00	杭州北京（现货）

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GNF-7

产品介绍

GNF-7 是一种多重激酶抑制剂。GNF-7 是 Bcr-Abl 的抑制剂，对 Bcr-Abl^WT 和 Bcr-Abl^T315I 作用的 IC₅₀ 值分别为 133 nM 和 61 nM。GNF-7 对 ACK1 和 GCK 也具有抑制活性，IC₅₀ 分别为 25 nM 和 8 nM。GNF-7 可用于血液恶性肿瘤的研究。

生物活性

GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC₅₀s of 133 nM and 61 nM for Bcr-Abl^WT and Bcr-Abl^T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC₅₀s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.

体外研究

GNF-7 potently inhibits wild-type Bcr-Abl (IC₅₀<5 nM) and Bcr-Abl mutants such as T315I (IC₅₀=11 nM), G250E (IC₅₀<5 nM), E255V (IC₅₀=10 nM), F317L (IC₅₀<5 nM) and M351T (IC₅₀<5 nM) in cellular assays.
GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream.
GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	Ba/F3-NRAS-G12D cells, OCI-AML3 cells
Concentration:	1 μM
Incubation Time:	2 hours
Result:	Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38.

Apoptosis Analysis

Cell Line:	OCI-AML3 cells
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1.

Cell Cycle Analysis

Cell Line:	OCI-AML3 cells
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Induced of G0-G1 arrest.

体内研究
(In Vivo)

GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model.
GNF-7 exhibits moderate oral bioavailability (mice 36%) and C_max (mice 3616 nM) following oral administration (mice 20 mg/kg).
GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Oral administration, daily, for 7 days
Result:	Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).

Animal Model:	5-6 weeks old male Balb/c mice (20-25 g)
Dosage:	5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral gavage
Result:	Oral bioavailability (36%), C_max (3616 nM), T_1/2 (3.2 h).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Oral administration, daily, for 7 days
Result:	Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).

Animal Model:	5-6 weeks old male Balb/c mice (20-25 g)
Dosage:	5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral gavage
Result:	Oral bioavailability (36%), C_max (3616 nM), T_1/2 (3.2 h).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Oral administration, daily, for 7 days
Result:	Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).

Animal Model:	5-6 weeks old male Balb/c mice (20-25 g)
Dosage:	5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral gavage
Result:	Oral bioavailability (36%), C_max (3616 nM), T_1/2 (3.2 h).

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 33 mg/mL (60.27 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8264 mL	9.1319 mL	18.2638 mL
5 mM	0.3653 mL	1.8264 mL	3.6528 mL
10 mM	0.1826 mL	0.9132 mL	1.8264 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (3.65 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.65 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2 mg/mL (3.65 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.65 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明