1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. SOS1-IN-14

SOS1-IN-14 是一种有效的、具有选择性和口服活性的 SOS1 抑制剂,IC50 值为 3.9 nM。SOS1-IN-14 可通过 P-糖蛋白介导的外排机制在肠道内被吸收。SOS1-IN-14 可用于研究 KRAS 突变的癌症。SOS1-IN-14 的抑瘤效果优于 BI-3406 (HY-125817)。

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SOS1-IN-14 Chemical Structure

SOS1-IN-14 Chemical Structure

CAS No. : 2793405-20-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥6710
In-stock
1 mg ¥2440
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5 mg ¥6100
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10 mg ¥9500
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100 mg   询价  

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Customer Review

查看 Ras 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817)[1].

IC50 & Target

IC50: 3.9 nM (SOS1)[1]

体外研究
(In Vitro)

SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC50 of 21 nM[1].
SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC50s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction[1].

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

体内研究
(In Vivo)

SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models[1].
SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles[1].
Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs[1].

ICR Mice Sprague–Dawley Rats Beagle Dogs
Administration p.o., 50 mg/kg i.v., 2 mg/kg p.o., 10 mg/kg i.v., 2 mg/kg p.o., 20 mg/kg
Tmax (h) 0.5 0.08 3 0.08 2
T1/2 (h) 4.61 1.17 2.32 3.83 6.68
Cmax (μg/mL) 2670 1261 265 568 1840
AUC0-24 (ng/mL·h) 32300 970 1683 2962 25725
CL (mL/min/kg) / 2068 / 11.3 /
Vss (L/kg) / 2126 / 3.88 /
F (%) / / 34.5 / 86.8
Kel (h-1) 0.265 / / / /
MRT (h) 4.67 / / / /

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

Animal Model: BALB/c nude mice (KRAS G12C variant Mia-paca-2 xenograft models)[1]
Dosage: 50 mg/kg
Administration: p.o.; q.d., for 21 days
Result: Exhibited 83.0% tumor suppression.
Showed better potent tumor suppression than BI-3406 (HY-125817).
分子量

550.57

Formula

C29H29F3N6O2

CAS 号
性状

固体

颜色

Light yellow to light brown

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 : 250 mg/mL (454.07 mM; 超声助溶; 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 1.8163 mL 9.0815 mL 18.1630 mL
5 mM 0.3633 mL 1.8163 mL 3.6326 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

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-14 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 1.8163 mL 9.0815 mL 18.1630 mL 45.4075 mL
5 mM 0.3633 mL 1.8163 mL 3.6326 mL 9.0815 mL
10 mM 0.1816 mL 0.9081 mL 1.8163 mL 4.5407 mL
15 mM 0.1211 mL 0.6054 mL 1.2109 mL 3.0272 mL
20 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
25 mM 0.0727 mL 0.3633 mL 0.7265 mL 1.8163 mL
30 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5136 mL
40 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1352 mL
50 mM 0.0363 mL 0.1816 mL 0.3633 mL 0.9081 mL
60 mM 0.0303 mL 0.1514 mL 0.3027 mL 0.7568 mL
80 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5676 mL
100 mM 0.0182 mL 0.0908 mL 0.1816 mL 0.4541 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.

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产品名称:
SOS1-IN-14
目录号:
HY-151517
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