CSF1R-IN-2 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CSF1R-IN-2 纯度: 99.97%

CSF1R-IN-2 (compound 5) 是 SRC，MET 和c-FMS 的口服有效抑制剂, 其对SRC，MET 和c-FMS 的 IC₅₀ 值分别为 0.12 nM，0.14 nM 和 0.76 nM。

CSF1R-IN-2 Chemical Structure

CAS No. : 2271119-26-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1760	In-stock
5 mg	￥1600	In-stock
10 mg	￥2300	In-stock
25 mg	￥4300	In-stock
50 mg	￥7400	In-stock
100 mg	￥12000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

CSF1R-IN-2 相关产品

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生物活性

CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC₅₀ values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively^[1].

IC₅₀ & Target

IC50: 0.12 nM (SRC), 0.14 nM (MET), 0.76 nM (c-FMS)^[1].

体外研究
(In Vitro)

CSF1R-IN-2 (compound 5) causes the suppression of MET autophosphorylation as well as the downstream STAT3, ERK and AKT phosphorylation at IC₅₀ values of around 1-3 nM in SNU-5 and MKN-45 cell lines^[1].

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.

体内研究
(In Vivo)

CSF1R-IN-2 (compound 5: p.o., BID, 13 days) treatment results in an 85% tumor regression and no body weight loss is observed after 21 days treatment in mice^[1].
CSF1R-IN-2 (compound 5: p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively in SCID/Beige mice^[1].
CSF1R-IN-2 (compound 5) inhibits MET activity in MKN-45 tumors following oral administration in mice^[1].

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:	Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model^[1].
Dosage:	15 mg/kg.
Administration:	PO, BID (twice daily) for 13 days.
Result:	Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment.

Animal Model:	SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm³^[1].
Dosage:	5 and 15 mg/kg.
Administration:	PO, BID (twice daily) for 10 days.
Result:	Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively.

分子量

409.42

Formula

C₂₀H₂₀FN₇O₂

CAS 号

2271119-26-5

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 : 25 mg/mL (61.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4425 mL	12.2124 mL	24.4248 mL
5 mM	0.4885 mL	2.4425 mL	4.8850 mL
10 mM	0.2442 mL	1.2212 mL	2.4425 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: ≥ 2.08 mg/mL (5.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.08 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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% corn oil

Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.08 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*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]. WO 2019023417 A1.

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