SOS1-IN-14|cas:2793405-20-4|西域试剂

SOS1-IN-14,99.38%

产品编号：Bellancom-151517| CAS NO：2793405-20-4| 分子式：C₂₉H₂₉F₃N₆O₂| 分子量：550.57

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-151517		￥6100.00	杭州北京（现货）
Bellancom-151517		￥9500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

SOS1-IN-14

产品介绍

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)。

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).

体外研究

SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC₅₀ of 21 nM.
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.

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

体内研究

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

	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
T_max (h)	0.5	0.08	3	0.08	2
T_1/2 (h)	4.61	1.17	2.32	3.83	6.68
C_max (μg/mL)	2670	1261	265	568	1840
AUC_0-24 (ng/mL·h)	32300	970	1683	2962	25725
CL (mL/min/kg)	/	2068	/	11.3	/
V_ss (L/kg)	/	2126	/	3.88	/
F (%)	/	/	34.5	/	86.8
K_el (h^-1)	0.265	/	/	/	/
MRT (h)	4.67	/	/	/	/

西域 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)
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).

体内研究

	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
T_max (h)	0.5	0.08	3	0.08	2
T_1/2 (h)	4.61	1.17	2.32	3.83	6.68
C_max (μg/mL)	2670	1261	265	568	1840
AUC_0-24 (ng/mL·h)	32300	970	1683	2962	25725
CL (mL/min/kg)	/	2068	/	11.3	/
V_ss (L/kg)	/	2126	/	3.88	/
F (%)	/	/	34.5	/	86.8
K_el (h^-1)	0.265	/	/	/	/
MRT (h)	4.67	/	/	/	/

西域 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)
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).

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (454.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8163 mL	9.0815 mL	18.1630 mL
5 mM	0.3633 mL	1.8163 mL	3.6326 mL
10 mM	0.1816 mL	0.9081 mL	1.8163 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式