GNF-7

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GNF-7  纯度: 98.93%

GNF-7 是一种多重激酶抑制剂。GNF-7 是 Bcr-Abl 的抑制剂，对 Bcr-AblWT 和 Bcr-AblT315I 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。

GNF-7

GNF-7 Chemical Structure

CAS No. : 839706-07-9

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10 mM * 1 mL in DMSO ￥1301 In-stock
5 mg ￥1080 In-stock
10 mg ￥1800 In-stock
25 mg ￥3500 In-stock
50 mg ￥6000 In-stock
100 mg ￥10500 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-AblWT and Bcr-AblT315I, 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[1][2][3].

IC50 & Target

IC50: 133 nM (Bcr-AblWT)[1], 61 nM (Bcr-AblT315I)[1], 25 nM (ACK1)[3], 8 nM (GCK)[3]
体外研究
(In Vitro)

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[2].
GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream[3].
GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

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[3]

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[3]

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[2].
GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg)[2].
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)[2].

上海金畔生物科技有限公司 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[2]
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)[2]
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%), Cmax (3616 nM), T1/2 (3.2 h).

分子量

547.53

Formula

C28H24F3N7O2
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。

    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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lu X, et al. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63.

    [2]. Choi HG, et al. A type-II kinase inhibitor capable of inhibiting the T315I “gatekeeper” mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48.

    [3]. Cho, H., et al. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. Journal of Medicinal Chemistry.

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