BRafV600E (IC50 = 0.6 nM); CRAF (IC50 = 5 nM); B-Raf (IC50 = 5.2 nM)

在 Raf 激酶选择性方面，达拉非尼对 B-Raf 的偏好程度超过 91% 的其他测试激酶的 400 倍。 Dabrafenib 通过最初将特异性编码 B-RafV600E 突变的癌细胞的细胞周期阻滞在 G1 期，减少 ERK 磷酸化并抑制细胞增殖。 [1]

Dabrafenib（口服）可抑制在免疫缺陷小鼠皮下生长的 B-RafV600E 突变结肠癌 (Colo205) 和黑色素瘤 (A375P) 人类肿瘤异种移植物的发育。 [1]

对于长期增殖测定，将细胞置于含有 10% FBS 的 RMPI-1640 中 12 天，并用单一化合物或化合物组合进行处理。该测定涉及至少一种化合物治疗替代。 12 天后，使用 50% 乙醇中的 0.5% 亚甲蓝对细胞进行染色。使用平板扫描仪拍摄照片。

The 26 10-week-old, time-mated, virus-antibody-free SD (Crl:CD[SD]) female rats that were chosen as the test system gave birth to the rat pups. From Day 20 to Day 23 postpartum, mated females are monitored for spontaneous deliveries (the day parturition is complete is designated PND 0). When parturition is complete, on PNDs 3 and 6, litter examinations are carried out. These examinations include external morphologic examinations, gender determination, and individual pup weights. Clinical signs and body weights are used to select parturient dams and their litters for the study, and chosen dams and their litters are then randomly assigned to study groups based on clinical observations and PND 3 litter mean body weights. On PND 3 or 4, litters are reduced to four or five males and females, with only a small amount of fostering required to achieve the desired sex ratio. This helps to preserve natural litter sizes as much as possible. Records of the pups raised by the original and foster dams are kept. Paw tattoos are used to identify each puppy. Nonlittermates are placed in subsets to the greatest extent possible. DAB is administered to young male and female rats by oral gavage at a dose volume of 5 ml/kg, based on daily body weight, in a suspension of vehicle, 0.5% hydroxypropylmethylcellulose K15M, and 0.1% (v/v) Tween80 in purified water.

[1]. Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.

[2]. Mol Cancer Ther . 2012 Apr;11(4):909-20.

[3]. ACS Med Chem Lett . 2013 Feb 7;4(3):358-62.

[4]. Clin Sci (Lond) . 2021 Jul 30;135(14):1631-1647.

C23H20F3N5O2S2

519.56

519.10

C, 53.17; H, 3.88; F, 10.97; N, 13.48; O, 6.16; S, 12.34

1195765-45-7

Dabrafenib Mesylate;1195768-06-9;Dabrafenib-d9;1423119-98-5

White to off-white solid powder

CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

BFSMGDJOXZAERB-UHFFFAOYSA-N

InChI=1S/C23H20F3N5O2S2/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25/h4-11,31H,1-3H3,(H2,27,28,29)

N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide

GSK2118436A; GSK-2118436B; GSK 2118436A; GSK2118436B (Dabrafenib Mesylate ); GSK-2118436A; GSK 2118436B. Trade name: Tafinlar

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

30% PEG400+0.5% Tween80+5% Propylene glycol: 8 mg/mL

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。