SBI-0640756
(Synonyms: SBI-756) 目录号 : GC19451
SBI-0640756 (SBI-756) 是 eIF4G1 的抑制剂，可破坏 eIF4F 复合物。
Cas No.:1821280-29-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | WM793, Lu1205, WM1346 and WM1366 melanoma cells are seeded at 1500 cells in 50 μL per well in 384-well plates. Cells are allowed to attach overnight. SBI-0640756 (SBI-756) or derivatives analogs are serially diluted 2-fold with media from stock solutions and added to cells. Tests are performed in triplicate, and each microplate included media and DMSO control wells. Cell viability is assessed using ATPlite after 48 or 72 h. Cell growth inhibition is calculated as a percentage of DMSO-treated controls and plotted against the log drug concentration. IC50 values are interpolated from the resulting linear regression curve fit[1]. |
Animal experiment: | Mice[1]Six-week-old female nu/nu mice are allowed to acclimatize for 1 week. A375 cells (1 × 106, suspended in 200 μL sterile PBS) are injected into subcutaneous flank tissue. When the xenograft size reach ∼250 mm3, mice are sorted into different groups. For PLX4720 and SBI-0640756 (SBI-756) combination experiments, mice are either fed PLX4720-containing chow alone (AIN76A Roden Diet with 417 mg PLX4720/kg) for the control group or PLX4720-containing chow plus an IP injection of 1 mg/kg SBI-0640756 twice a week. For MEKi plus SBI-0640756 (SBI-756) experiments, PD0325901 at 20 mg/kg (formulated in 0.5% hydroxypropyl methylcellulose plus 0.2% Tween-80) is administered by oral gavage twice a week (Monday and Thursday) for the control group, or PD035901 plus IP injection of 1 mg/kg SBI-0640756 (SBI-756) is administered twice a week (Tuesday and Friday)[1]. |
References: [1]. Feng Y et al. SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex. Cancer Res, 2015 Dec 15, 75(24):5211-8. | |
SBI-0640756 is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.
SBI-0640756 is a water soluble inhibitor of eIF4G1. SBI-0640756 (0-1 μM) disrupts eIF4F complex in parent and BRAFi-resistant melanoma. SBI-0640756 shows inhibitory effect on human melanoma lines, and also suppresses AKT, NF-κB and AKT/mTORC1 activity[1].
SBI-0640756 (0.5 mg/kg, i.p.) delays tumor onset and reduces tumor incidence by 50% in NrasQ61K/Ink4a-/- genetic model. SBI-0640756 (1 mg/kg, 2 times per week, i.p.) in combination with BRAF inhibitor potently suppresses growth of established tumors and does not resume tumor growth in immunodeficient mice bearing A375 tumors[1].
[1]. Feng Y et al. SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex. Cancer Res, 2015 Dec 15, 75(24):5211-8.
| Cas No. | 1821280-29-8 | SDF | |
| 别名 | SBI-756 | ||
| Canonical SMILES | O=C1C(C(/C=C/C2=CC(F)=CN=C2)=O)=C(C3=CC=CC=C3)C4=C(C=CC(Cl)=C4)N1 | ||
| 分子式 | C23H14ClFN2O2 | 分子量 | 404.82 |
| 溶解度 | DMSO : ≥ 26 mg/mL (64.23 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 | 2.4702 mL | 12.3512 mL | 24.7023 mL |
| 5 mM | 0.494 mL | 2.4702 mL | 4.9405 mL |
| 10 mM | 0.247 mL | 1.2351 mL | 2.4702 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。