Name: Tunlametinib
Brand: TargetMol
SKU: T39220
Price: 346 CNY
Availability: InStock
Rating: 5 (10 reviews)

Tunlametinib

很棒

产品编号 T39220Cas号 1801756-06-8

别名 妥拉美替尼, HL-085, HL085

Tunlametinib是高选择性口服MEK1/MEK2激酶抑制剂（对MEK1的IC50为1.9 nM），通过阻断RAS-RAF-MEK-ERK致癌信号通路诱导肿瘤细胞周期阻滞与凋亡。对BRAF V600E或KRAS G12C等突变型肿瘤细胞具有强抑制活性，与BRAF/KRASG12C/SHP2抑制剂及多西他赛（Docetaxel）联用呈现协同效应，目前已应用于黑色素瘤、结直肠癌及非小细胞肺癌等RAS/RAF驱动型肿瘤的靶向治疗。

规格

价格

库存

数量

1 mg

¥ 346

In stock

5 mg

¥ 823

In stock

10 mg

¥ 1,290

In stock

1 mL x 10 mM (in DMSO)

¥ 888

In stock

产品介绍

生物活性

产品描述	Tunlametinib is a highly selective, orally bioavailable small molecule inhibitor of MEK1 and MEK2 kinases with a reported IC50 value of 1.9 nM for MEK1. Tunlametinib exerts its antitumor effects by blocking the oncogenic RAS-RAF-MEK-ERK signaling pathway, thereby inducing tumor cell cycle arrest and promoting apoptosis, Tunlametinib demonstrates strong inhibitory activity against various RAS/RAF-mutant cancer cells such as those harboring BRAF V600E or KRAS G12C mutations, shows synergistic effects in combination with BRAF/KRASG12C/SHP2 inhibitors and Docetaxel, and is used in targeted therapy for RAS/RAF-driven cancers including melanoma, colorectal cancer, and non-small cell lung cancer (NSCLC).
靶点活性	HT-291 cells:10.07 nM, Colo-829 cells:3.46 nM, A375 cells:0.86 nM, COLO 205 cells:0.94 nM, HL-60 cells:0.67 nM, A549 cells:59.89 nM
体外活性	方法：Tunlametinib (1-9 nM，48 h) 处理 A375 细胞，评估对细胞周期的影响。结果：Tunlametinib可以剂量依赖性增加 A375 细胞在 G0/G1 期的细胞比例，并且诱导细胞周期阻滞。方法：Tunlametinib 处理BRAF/KRAS 突变细胞系：A375、Colo-829、HL-60 黑色素瘤细胞，COLO 205、HT-29 结肠癌细胞，Calu-6，A549 肺癌细胞，MTS法测定细胞活力。结果：Tunlametinib 在上述细胞中的IC50值为 0.86 nM，3.46 nM，0.67 nM，0.94 nM，10.07 nM，59.89 nM。[1]
体内活性	方法：Tunlametinib (1、3、6 mg/kg，口服，每日 1 次，21 天) 处理雌性 BALB/c 裸鼠、NU/NU 或 Nod-Scid 小鼠的 A375 (BRAF V600E 突变黑色素瘤)、COLO 205 (BRAF V600E突变结肠癌)、Calu-6 (KRAS Q61K突变肺癌) 荷瘤模型小鼠，观察体内肿瘤情况。结果：Tunlametinib可以抑制上述小鼠体内的肿瘤生长，并且呈浓度依赖式。[1]
别名	妥拉美替尼, HL-085, HL085

化学信息

分子量	491.25
分子式	C₁₆H₁₂F₂IN₃O₃S
CAS No.	1801756-06-8
Smiles	O=C(NOCCO)C1=CC=2SC=NC2C(F)=C1NC3=CC=C(I)C=C3F
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 80 mg/mL (162.85 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0356 mL	10.1781 mL	20.3562 mL	101.7812 mL
5 mM	0.4071 mL	2.0356 mL	4.0712 mL	20.3562 mL
10 mM	0.2036 mL	1.0178 mL	2.0356 mL	10.1781 mL
20 mM	0.1018 mL	0.5089 mL	1.0178 mL	5.0891 mL
50 mM	0.0407 mL	0.2036 mL	0.4071 mL	2.0356 mL
100 mM	0.0204 mL	0.1018 mL	0.2036 mL	1.0178 mL

体内实验配液计算器