MRTX0902|cas:2654743-22-1|西域试剂

MRTX0902,99.45%

产品编号：Bellancom-145926| CAS NO：2654743-22-1| 分子式：C₂₂H₂₄N₆O| 分子量：388.47

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-145926		￥4200.00	杭州北京（现货）
Bellancom-145926		￥6800.00	杭州北京（现货）

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MRTX0902

产品介绍

MRTX0902 是一种口服有效的 SOS1 的抑制剂，IC₅₀ 为 46 nM。

生物活性

MRTX0902 is an orally active and potent SOS1 inhibitor with an IC₅₀ of 46 nM (WO2021127429A1; Example 12-10).

体外研究

MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) shows a moderate Cl_int value of 195 mL/min/kg in human liver microsome and a low lipophilicity with cLogP of 3.4.
MRTX0902 displays high selectivity on SOS1 (K_i=2 nM) over SOS2 and EGFR (both K_i values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC₅₀ value of 29 nM.

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

体内研究

MRTX0902 (compound 32) (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression.
MRTX0902 (1-3 mg/kg for i.v. or 10-30 mg/kg for p.o.; single dose) exhibits good brain penetrance, low clearance, and high bioavailability.
PK Parameters for MRTX0902 across Species

Parameter	Route	Dose (mg/kg)	Cl (mL/min/kg)	V_d,ss (L/kg)	T_1/2(iv) (h)	F (%)
Mouse	IV/PO	3/30	4.4	0.28	1.3	69
Rat	IV/PO	1/10	14.6	0.28	0.62	83
Dog	IV/PO	2/10	7.6	0.48	0.86	38

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

Animal Model:	Female CD-1 mice
Dosage:	50 mg/kg
Administration:	Oral gavage; twice daily; 1 day
Result:	Resulted free drug exposure in the brain as well as the efflux ratio in the Caco-2 assay (ER = 1.5). Showed short half-life of the compound in mice (T_1/2 = 1.3 h).

Animal Model:	MIA PaCa-2 xenograft model in mouse
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Oral gavage; twice daily; 25 days
Result:	Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration.

体内研究

Parameter	Route	Dose (mg/kg)	Cl (mL/min/kg)	V_d,ss (L/kg)	T_1/2(iv) (h)	F (%)
Mouse	IV/PO	3/30	4.4	0.28	1.3	69
Rat	IV/PO	1/10	14.6	0.28	0.62	83
Dog	IV/PO	2/10	7.6	0.48	0.86	38

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

Animal Model:	Female CD-1 mice
Dosage:	50 mg/kg
Administration:	Oral gavage; twice daily; 1 day
Result:	Resulted free drug exposure in the brain as well as the efflux ratio in the Caco-2 assay (ER = 1.5). Showed short half-life of the compound in mice (T_1/2 = 1.3 h).

Animal Model:	MIA PaCa-2 xenograft model in mouse
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Oral gavage; twice daily; 25 days
Result:	Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (32.18 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5742 mL	12.8710 mL	25.7420 mL
5 mM	0.5148 mL	2.5742 mL	5.1484 mL
10 mM	0.2574 mL	1.2871 mL	2.5742 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.22 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.22 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明