SYN1143|cas:913376-84-8|西域试剂

SYN1143,99.36%

产品编号：Bellancom-18307| CAS NO：913376-84-8| 分子式：C₃₁H₂₉FN₄O₅| 分子量：556.58

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货号	价格	库存与货期
Bellancom-18307	￥2000.00	杭州北京（现货）
Bellancom-18307	￥3200.00	杭州北京（现货）
Bellancom-18307	￥6400.00	杭州北京（现货）
Bellancom-18307	￥10300.00	杭州北京（现货）

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SYN1143

产品介绍

SYN1143 是一种有效，选择性和具有口服活性的 c-Met/RON 的双重抑制剂，IC₅₀ 值分别为 4 和 9 nM。SYN1143 对 Lck，Tie2，Src 和 BTK 的抑制活性较弱，IC₅₀ 值为 160 至 710 nM。SYN1143 可用于癌症的研究。

生物活性

SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC₅₀s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC₅₀s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.

体外研究

SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells.
SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells.
SYN1143 (0.3-30 μM; 2 h or 3 d) inhibits c-Met signaling and cell proliferation in MC₃T₃-E₁ and C₃H₁₀T_1/2 cells.
SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells.

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

Western Blot Analysis

Cell Line:	HT-29 and BxPC3 cells
Concentration:	10, 30, 100, 300, 1000 nM
Incubation Time:	1 hours
Result:	Inhibited HGF-mediated c-Met phosphorylation and downstream signaling in a dose-dependent manner in both cell lines.

体内研究
(In Vivo)

SYN1143 (10-100 mg/kg; p.o. for 22 d) inhibits the growth of c-Met-dependent and constitutively active RON-expressing tumors in mice.
SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone.

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

Animal Model:	Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s.c. tumors
Dosage:	10, 30, 100 mg/kg
Administration:	Oral gavage either once or twice daily for 22 days
Result:	Significantly inhibited tumor growth at doses of 30 or 100 mg/kg once daily or at 30 mg/kg twice daily. Completely inhibited tumor growth at a dose of 100 mg/kg once daily. Did not adversely affect body weight.

体内研究

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

Animal Model:	Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s.c. tumors
Dosage:	10, 30, 100 mg/kg
Administration:	Oral gavage either once or twice daily for 22 days
Result:	Significantly inhibited tumor growth at doses of 30 or 100 mg/kg once daily or at 30 mg/kg twice daily. Completely inhibited tumor growth at a dose of 100 mg/kg once daily. Did not adversely affect body weight.

体内研究

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

Animal Model:	Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s.c. tumors
Dosage:	10, 30, 100 mg/kg
Administration:	Oral gavage either once or twice daily for 22 days
Result:	Significantly inhibited tumor growth at doses of 30 or 100 mg/kg once daily or at 30 mg/kg twice daily. Completely inhibited tumor growth at a dose of 100 mg/kg once daily. Did not adversely affect body weight.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (179.67 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7967 mL	8.9834 mL	17.9669 mL
5 mM	0.3593 mL	1.7967 mL	3.5934 mL
10 mM	0.1797 mL	0.8983 mL	1.7967 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 (4.49 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.49 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 (4.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.49 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 (4.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.49 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。