GNF-7 - CAS:839706-07-9

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GNF-7

目录号 : KM4962 CAS No. : 839706-07-9 纯度 : 98%

Data Sheet 产品使用指南

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。

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25mg		In-stock
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100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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 and Bcr-Abl, 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.

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

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).

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).

分子式

C₂₈H₂₄N₇O₂F₃

分子量

547.53

CAS号

839706-07-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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。
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。