SOS1-IN-15|cas:2793404-47-2|西域试剂

SOS1-IN-15

产品编号：Bellancom-151881| CAS NO：2793404-47-2| 分子式：C₂₈H₂₇F₃N₆O₂| 分子量：536.55

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-151881		￥4500.00	杭州北京（现货）
Bellancom-151881		￥8000.00	杭州北京（现货）

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SOS1-IN-15

产品介绍

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。

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.

体外研究

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).
SOS1-IN-15 has a limited inhibition of CYP and hERG.

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

Cell Proliferation Assay

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.

西域 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
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

Dosage:

20 mg/kg

Administration:

Oral administration (Pharmacokinetic Analysis)

Result:

In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 Mice^a

	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC (ng⋅h/mL)	MRT (h)	K_el (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: T_1/2, elimination half-life; T_max, plasma peak time after administration; C_max, maximum plasma concentration; AUC, area under concentration-time curve. MRT, mean residence time; K_el, elimination rate constant.

体内研究

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

西域 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
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

Dosage:

20 mg/kg

Administration:

Oral administration (Pharmacokinetic Analysis)

Result:

In Vivo Pharmacokinetic Properties of the Compounds in Male CD-1 Mice^a

	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC (ng⋅h/mL)	MRT (h)	K_el (h^-1)
SOS1-IN-15	11.4	3.67	1550	9900	4.19	0.25

体内研究

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

西域 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
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.