2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. SOS1-IN-15

SOS1-IN-15 (Compound 37) 是一种具有口服活性的 SOS1 抑制剂，IC50 为 5 nM。SOS1-IN-15 可用于 KRAS 驱动型癌症研究。

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SOS1-IN-15 Chemical Structure

SOS1-IN-15 Chemical Structure

CAS No. : 2793404-47-2

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SOS1-IN-15 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer[1].

IC50 & Target[1]

SOS1

5 nM (IC50)

体外研究
(In Vitro)

SOS1-IN-15 (Compound 37) (0.1 nM-0.1 mM; 72 h) displays prominent inhibitory activities in Mia-paca-2 cancer cells (IC50 = 178 ± 42 nM)[1].
SOS1-IN-15 has a limited inhibition of CYP and hERG[1].

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

SOS1-IN-15 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Mia-paca-2 pancreas cancer cells
Concentration: 0.1 nM-0.1 mM
Incubation Time: 72 h
Result: Inhibited the proliferation with an IC50 of 178 ± 42 nM.
体内研究
(In Vivo)

SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice[1].

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

Animal Model: BALB/c nude mice bearing Mia-paca-2 pancreas tumors[1]
Dosage: 50 mg/kg
Administration: Oral administration, daily for 22 days
Result: Showed 49% tumor inhibition. No animal mortality and significant difference in the mice’s body weight were observed during the study period.
Animal Model: Male CD-1 Mice[1]
Dosage: 20 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 Micea
T1/2 (h) Tmax (h) Cmax (ng/mL) AUC (ng⋅h/mL) MRT (h) Kel (h-1)
SOS1-IN-15 11.4 3.67 1550 9900 4.19 0.25

aCompounds (20 mg/kg) were P.O. dosed in a mixture of 63% water + 30% PEG +5 % DMSO + 2% Tween 80 in male ICR mice (n = 3). Abbreviations: T1/2, elimination half-life; Tmax, plasma peak time after administration; Cmax, maximum plasma concentration; AUC, area under concentration-time curve. MRT, mean residence time; Kel, elimination rate constant.
分子量

536.55

Formula

C28H27F3N6O2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 5 mg/mL (9.32 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8638 mL 9.3188 mL 18.6376 mL
5 mM 0.3728 mL 1.8638 mL 3.7275 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

SOS1-IN-15 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8638 mL 9.3188 mL 18.6376 mL 46.5940 mL
5 mM 0.3728 mL 1.8638 mL 3.7275 mL 9.3188 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SOS1-IN-152793404-47-2Rasorally activeKRAS-driven cancerMia-paca-2BALB/c nude miceInhibitorinhibitorinhibit

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目录号：
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