Opnurasib JDQ-443; NVP-JDQ443|cas:2653994-08-0|西域试剂

Opnurasib JDQ-443; NVP-JDQ443,98.94%

产品编号：Bellancom-139612| CAS NO：2653994-08-0| 分子式：C₂₉H₂₈ClN₇O| 分子量：526.03

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	价格	库存与货期
Bellancom-139612	￥3800.00	杭州北京（现货）
Bellancom-139612	￥6080.00	杭州北京（现货）
Bellancom-139612	￥10500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Opnurasib JDQ-443; NVP-JDQ443

产品介绍

Opnurasib (JDQ-443) (NVP-JDQ443) 是一种口服有效和选择性的共价 KRAS G12C 抑制剂。Opnurasib 具有抗肿瘤活性。

生物活性

Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.

体外研究

Opnurasib (NVP-JDQ443) traps the GDP-bound inactive conformation of KRAS.
Opnurasib promotes dose-dependent reductions of phosphorylated ERK (pERK) levels and the proliferation of the KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, with IC₅₀ values of 0.018 and 0.063 μM, respectively.
Opnurasib covalently and selectively binds and inhibits GDP-bound KRASG12C with low reversible binding affinity to the RAS switch II pocket, and also inhibits proliferation of KRASG12C-mutated and KRAS G12C/H95, G12C/R68S, and G12C/Y96 double-mutant cell lines.

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

Western Blot Analysis

Cell Line:	Ba/F3 cells
Concentration:	0, 0.3, 1 μM
Incubation Time:	30 min, 4 h
Result:	Inhibited signaling (pERK) and proliferation of the KRAS G12C/H95 double mutants G12C/H95R and G12C/H95Q.

体内研究
(In Vivo)

Opnurasib (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity in KRAS G12C-mutated CDX models.
Opnurasib (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155.
Opnurasib generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents.

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

Animal Model:	KRAS G12C tumor-bearing nude mice (MIA PaCa-2 (PDAC); NCIH2122, LU99, HCC44, NCI-H2030 (NSCLC); and KYSE410 (esophageal cancer))
Dosage:	10, 30, 100 mg/kg
Administration:	Orally, daily for 14 days
Result:	Inhibited the growth of all models in a dose-dependent manner.

Animal Model:	Three KRAS G12C-mutated CDX models (LU99, NCI-H2030, and KYSE410)
Dosage:	100 mg/kg (JDQ443) + 7.5 mg/kg (TNO155)
Administration:	Orally, daily (JDQ443) or twice daily (TNO155), for 36 days
Result:	Combined with TNO155, showed either greater tumor efficacy compared with each agent alone (H2030, KYSE410) or a delayed time to tumor progression (LU99).

体内研究

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

Animal Model:	KRAS G12C tumor-bearing nude mice (MIA PaCa-2 (PDAC); NCIH2122, LU99, HCC44, NCI-H2030 (NSCLC); and KYSE410 (esophageal cancer))
Dosage:	10, 30, 100 mg/kg
Administration:	Orally, daily for 14 days
Result:	Inhibited the growth of all models in a dose-dependent manner.

Animal Model:	Three KRAS G12C-mutated CDX models (LU99, NCI-H2030, and KYSE410)
Dosage:	100 mg/kg (JDQ443) + 7.5 mg/kg (TNO155)
Administration:	Orally, daily (JDQ443) or twice daily (TNO155), for 36 days
Result:	Combined with TNO155, showed either greater tumor efficacy compared with each agent alone (H2030, KYSE410) or a delayed time to tumor progression (LU99).

体内研究

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

Animal Model:	KRAS G12C tumor-bearing nude mice (MIA PaCa-2 (PDAC); NCIH2122, LU99, HCC44, NCI-H2030 (NSCLC); and KYSE410 (esophageal cancer))
Dosage:	10, 30, 100 mg/kg
Administration:	Orally, daily for 14 days
Result:	Inhibited the growth of all models in a dose-dependent manner.

Animal Model:	Three KRAS G12C-mutated CDX models (LU99, NCI-H2030, and KYSE410)
Dosage:	100 mg/kg (JDQ443) + 7.5 mg/kg (TNO155)
Administration:	Orally, daily (JDQ443) or twice daily (TNO155), for 36 days
Result:	Combined with TNO155, showed either greater tumor efficacy compared with each agent alone (H2030, KYSE410) or a delayed time to tumor progression (LU99).

性状

Solid

溶解性数据

In Vitro:

DMSO : 80 mg/mL (152.08 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9010 mL	9.5052 mL	19.0103 mL
5 mM	0.3802 mL	1.9010 mL	3.8021 mL
10 mM	0.1901 mL	0.9505 mL	1.9010 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。