GNF-5|cas:778277-15-9|西域试剂

GNF-5,99.42%

产品编号：Bellancom-15738| CAS NO：778277-15-9| 分子式：C₂₀H₁₇F₃N₄O₃| 分子量：418.37

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-15738	￥500.00	杭州北京（现货）
Bellancom-15738	￥1485.00	杭州北京（现货）
Bellancom-15738	￥2100.00	杭州北京（现货）

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GNF-5

产品介绍

GNF-5 是 GNF-2 的 n -羟乙基羧酰胺类似物，是一种 Bcr-Abl 抑制剂，具有口服活性。GNF-5 具有 Bcr-Abl 抑制活性，其IC₅₀ 值为 0.22 μ M。GNF-5 具有良好的药代动力学特性。GNF-5 可用于多种癌症如慢性粒细胞白血病 (Chronic myelogenous leukemia, CML) 和乳腺癌的研究。

生物活性

GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC₅₀ value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.

体外研究

GNF-5 has inhibition of wild-type Abl with an IC₅₀ value of 0.22 µM but no inhibition for myristate site mutant E505K (IC₅₀ ＞10 µM).

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

Cell Viability Assay

Cell Line:	wild type and mutant Bcr-Abl expressing Ba/F3 cells
Concentration:	0.2, 0.8 and 1.6 μM
Incubation Time:	48 h
Result:	Inhibited wild-type Abl in a non-ATP competitive fashion.

体内研究
(In Vivo)

GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters.
GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses.
GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo.

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

Animal Model:

Male Balb/c mice

Dosage:

5 mg/kg, 20 mg/kg

Administration:

5 mg/kg intravenously or 20 mg/kg orally

Result:

AUC_inf (min*ug/mL)	292.37
AUC_inf (hrs*nM	11647
C_max(nM)	4386.08
T_max(hrs)	0.50
Clast (nM)	636.16
T_1/2(hrs)	2.30
V_ss(L/kg)	9.18
F (%)	44.82

Animal Model:	p210 xenograft model
Dosage:	50 or 100 mg/kg
Administration:	oral, twice daily, for 7 days
Result:	Could normalize blood counts and spleen size.

Animal Model:	Bone marrow transduction/transplantation model
Dosage:	75 mg/kg
Administration:	twice daily
Result:	Showed no significant response (alone). Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.

体内研究

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

Animal Model:

Male Balb/c mice

Dosage:

5 mg/kg, 20 mg/kg

Administration:

5 mg/kg intravenously or 20 mg/kg orally

Result:

AUC_inf (min*ug/mL)	292.37
AUC_inf (hrs*nM	11647
C_max(nM)	4386.08
T_max(hrs)	0.50
Clast (nM)	636.16
T_1/2(hrs)	2.30
V_ss(L/kg)	9.18
F (%)	44.82

Animal Model:	p210 xenograft model
Dosage:	50 or 100 mg/kg
Administration:	oral, twice daily, for 7 days
Result:	Could normalize blood counts and spleen size.

Animal Model:	Bone marrow transduction/transplantation model
Dosage:	75 mg/kg
Administration:	twice daily
Result:	Showed no significant response (alone). Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.

体内研究

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

Animal Model:

Male Balb/c mice

Dosage:

5 mg/kg, 20 mg/kg

Administration:

5 mg/kg intravenously or 20 mg/kg orally

Result:

AUC_inf (min*ug/mL)	292.37
AUC_inf (hrs*nM	11647
C_max(nM)	4386.08
T_max(hrs)	0.50
Clast (nM)	636.16
T_1/2(hrs)	2.30
V_ss(L/kg)	9.18
F (%)	44.82

Animal Model:	p210 xenograft model
Dosage:	50 or 100 mg/kg
Administration:	oral, twice daily, for 7 days
Result:	Could normalize blood counts and spleen size.

Animal Model:	Bone marrow transduction/transplantation model
Dosage:	75 mg/kg
Administration:	twice daily
Result:	Showed no significant response (alone). Showed no toxicity and had a strong and sustained inhibition of Bcr-Abl-mediated signaling combination with nilotinib.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 49 mg/mL (117.12 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	2.3902 mL	11.9511 mL	23.9023 mL
5 mM	0.4780 mL	2.3902 mL	4.7805 mL
10 mM	0.2390 mL	1.1951 mL	2.3902 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: ≥ 2.5 mg/mL (5.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.98 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.98 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。