1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Theliatinib

Theliatinib (Synonyms: 西利替尼; Xiliertinib; HMPL-309)

目录号: HY-104066 纯度: 99.88%
产品使用指南

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,Ki 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。抗肿瘤活性。

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Theliatinib Chemical Structure

Theliatinib Chemical Structure

CAS No. : 1353644-70-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1947
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1 mg ¥680
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5 mg ¥2000
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10 mg ¥3250
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25 mg ¥6500
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50 mg ¥11000
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100 mg ¥19000
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki 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. Anti-tumor activity[1].

IC50 & Target[1]

EGFR

3 nM (IC50)

EGFR

0.05 nM (Ki)

EGFR (L858R/T790M)

22 nM (IC50)

体外研究
(In Vitro)

Theliatinib significantly inhibits EGFR phosphorylation in A431 cells with an IC50 of 7 nM. Theliatinib also inhibits A431, H292 and FaDu cells survival with IC50 values of 80 nM, 58 nM and 354 nM, respectively[1].

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

体内研究
(In Vivo)

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[1].

MCE 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)[1]
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.
Clinical Trial
分子量

442.51

Formula

C25H26N6O2

CAS 号
中文名称

西利替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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