Theliatinib 西利替尼; Xiliertinib; HMPL-309|cas:1353644-70-8|西域试剂

Theliatinib 西利替尼; Xiliertinib; HMPL-309,99.77%

产品编号：Bellancom-104066| CAS NO：1353644-70-8| 分子式：C₂₅H₂₆N₆O₂| 分子量：442.51

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货号	价格	库存与货期
Bellancom-104066	￥680.00	杭州北京（现货）
Bellancom-104066	￥2000.00	杭州北京（现货）
Bellancom-104066	￥3250.00	杭州北京（现货）
Bellancom-104066	￥6500.00	杭州北京（现货）
Bellancom-104066	￥11000.00	杭州北京（现货）

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Theliatinib 西利替尼; Xiliertinib; HMPL-309

产品介绍

Theliatinib (Xiliertinib) 是一种有效、ATP 竞争性、口服活性和高度选择性的 EGFR 抑制剂，K_i 为 0.05 nM，IC₅₀ 为 3 nM。Theliatinib 对 EGFR T790M/L858R 突变体的 IC₅₀ 值为 22 nM。Theliatinib 对 EGFR 的选择性是其他激酶的 50 倍以上。

生物活性

Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases.

体外研究

Theliatinib 显着抑制 A431 细胞中的 EGFR 磷酸化，IC₅₀ 为 7 nM。Theliatinib 还抑制 A431、H292 和 FaDu 细胞存活，IC₅₀ 值分别为 80 nM、58 nM 和 354 nM。

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

体内研究

Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response.

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

Animal Model:	NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)
Dosage:	2 mg/kg, 5 mg/kg, 15 mg/kg
Administration:	Oral administration;daily; for 21 days
Result:	Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.

体内研究

Theliatinib (2-15 mg/kg; oral administration;daily; for 21 days; NOD-SCID mice; PDECX 1T0950 model) treatment demonstrates tumor regression of 75% at the end of study, and with a dose response.

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

Animal Model:	NOD-SCID mice injected with esophageal cancer cells (PDECX 1T0950 model)
Dosage:	2 mg/kg, 5 mg/kg, 15 mg/kg
Administration:	Oral administration;daily; for 21 days
Result:	Attenuated tumor growth in PDECX 1T0950 model in a dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (11.30 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2598 mL	11.2992 mL	22.5984 mL
5 mM	0.4520 mL	2.2598 mL	4.5197 mL
10 mM	0.2260 mL	1.1299 mL	2.2598 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