GGTI298 Trifluoroacetate
目录号 : GC19164
GGTI298 Trifluoroacetate是一种选择性、不可逆的香叶基香叶酰转移酶I（GGTase-I）抑制剂（IC50 = 3μM)。
Cas No.:1217457-86-7
Sample solution is provided at 25 µL, 10mM.
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GGTI298 Trifluoroacetate is a selective, irreversible inhibitor of geranylgeranyl transferase I (GGTase-I) (IC50 = 3μM) [1]. By inhibiting GGTase-I, GGTI298 Trifluoroacetate blocks geranylgeranylation of small GTPases such as RhoA, leading to cell cycle arrest at the G0/G1 phase and induction of apoptosis [2-3]. GGTI298 Trifluoroacetate is primarily used to treat non-small cell lung cancer [4].
In A549 cells, Gefitinib and GGTI298 Trifluoroacetate (2.5-5µM; 48h) have synergistic anti-proliferative effects on cells [5]. In A549 cells, GGTI298 Trifluoroacetate (15µM; 48h) induces cell apoptosis [6].
In Luc-G33 cells xenograft mice model, combination treatment with Zoledronate and GGTI298 Trifluoroacetate (1.16mg/kg; sc; 35d) both reduced tumor growth [7].
References:
[1]. Dan H C, Jiang K, Coppola D, et al. GGTI 298[J]. Oncogene, 2004, 23: 706-715.
[2]. Peterson Y K, Kelly P, Weinbaum C A, et al. A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity[J]. Journal of Biological Chemistry, 2006, 281(18): 12445-12450.
[3]. Vogt A, Sun J, Qian Y, et al. The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21WAF1/CIP1/SDI1 in a p53-independent manner[J]. Journal of Biological Chemistry, 1997, 272(43): 27224-27229.
[4]. Chen S, Fu L, Raja S M, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis[J]. Molecular cancer, 2010, 9(1): 23.
[5]. Liu B S, Dai X Y, Xia H W, et al. Geranylgeranyl transferase 1 inhibitor GGTI-298 enhances the anticancer effect of gefitinib[J]. Molecular Medicine Reports, 2018, 18(4): 4023-4029.
[6]. Miquel K, Pradines A, Sun J, et al. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells[J]. Cancer research, 1997, 57(10): 1846-1850.
[7]. Lau C P Y, Wong K C, Huang L, et al. A mouse model of luciferase-transfected stromal cells of giant cell tumor of bone[J]. Connective tissue research, 2015, 56(6): 493-503.
GGTI298 Trifluoroacetate是一种选择性、不可逆的香叶基香叶酰转移酶I（GGTase-I）抑制剂（IC50 = 3μM) [1]。通过抑制GGTase-I，GGTI298 Trifluoroacetate可阻断RhoA等小GTP酶的香叶基香叶酰化修饰，导致细胞周期停滞于G0/G1期并诱导细胞凋亡 [2-3]。GGTI298 Trifluoroacetate主要用于治疗非小细胞肺癌 [4]。
在A549细胞中，gefitinib和GGTI298 Trifluoroacetate（2.5-5μM；48h）具有协同抗增殖作用 [5]。在A549细胞中，GGTI298 Trifluoroacetate（15μM；48h）可诱导细胞凋亡 [6]。
在Luc-G33细胞异种移植小鼠模型中，zoledronate和GGTI298 Trifluoroacetate（1.16mg/kg；sc；35d）联合治疗均能降低肿瘤增长 [7]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were seeded (5×103 cells per well in 100µL DMEM with 10% FBS) in a 96-well flat-bottomed plate at 24h prior to treatment. A549 cells were treated with gefitinib (5µM) and/or GGTI298 Trifluoroacetate (concentration indicated) for 48h at 37℃ in a humidified (5% CO2, 95% air) incubator. Following incubation at 37℃, cell growth was measured using a Cell Counting Kit-8. |
Reaction Conditions | 2.5-5µM; 48h |
Applications | Gefitinib and GGTI298 Trifluoroacetate have synergistic anti-proliferative effects on cells. |
| Animal experiment [2]: | |
Animal models | Luc-G33 cells xenograft mice model |
Preparation Method | The nude mice were initially weighed and anesthetized intraperitoneally with 10% chloral hydrate at 0.1ml/30g live weight. The operative area was prepared with iodine. Each mouse was then given an intraosseous (1×106) and a subcutaneous injection (3×106) of Luc-G33 cells in hydrogel into the tibia and under the dorsal skin, respectively. A preliminary study had been proceeded on eight mice for observing the duration of the BLI signals from the Luc-G33 cells in the mice in vivo. Thirty-two mice after Luc-G33 implantation were randomly divided into four groups (8 mice/group) with equal average body weight and drugs were given to each mice three days after cell injection. Group 1 was then given 0.9% sodium chloride (Abbott) as the vehicle control treatment; Groups 2–4 were given Zoledronate (ZOL) and GGTI298 Trifluoroacetate treatments at the following dosages: group 2 treated with ZOL alone at 400mg/kg; group 3 with GGTI298 Trifluoroacetate alone at 1.16mg/kg; and group 4 with the combination of ZOL at 400mg/kg and GGTI298 Trifluoroacetate at 1.16mg/kg. |
Dosage form | 1.16mg/kg; sc; 35d |
Applications | Combination treatment with Zoledronate and GGTI298 Trifluoroacetate both reduced tumor proliferation. |
References: | |
| Cas No. | 1217457-86-7 | SDF | |
| Canonical SMILES | CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O.O=C(O)C(F)(F)F | ||
| 分子式 | C29H34F3N3O5S | 分子量 | 593.66 |
| 溶解度 | DMSO : 150 mg/mL (252.67 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6845 mL | 8.4223 mL | 16.8447 mL |
| 5 mM | 336.9 μL | 1.6845 mL | 3.3689 mL |
| 10 mM | 168.4 μL | 842.2 μL | 1.6845 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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