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^[1].

SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells^[1].
SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells^[1].
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^[2].
SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells^[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.

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^[1].
SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone^[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.

556.58

C₃₁H₂₉FN₄O₅

913376-84-8

Room temperature in continental US; may vary elsewhere.

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

In Vitro: 

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

*

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。

• [1]. Zhang Y, et, al. Identification of a novel recepteur d’origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7.

  [2]. Kim JW, et, al. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur J Pharmacol. 2017 Jul 5;806:10-17.