ALLO-1
目录号 : GC14749
A smoothened antagonist
Cas No.:37468-32-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 50 nM for wile type Smo
ALLO-1 is a SMO antagonist.
Hedgehog (Hh) proteins are important development regulators that bind the cell-surface protein, which allows the activation of a GPCR-like receptor, Smoothened (SMO). In vertebrates, the SMO activation finally results in the activation of the zinc-finger transcription factors of the Gli family. In addition, the overactivation of SMO may lead to certain cancers.
In vitro: Previous study found that ALLO-1 and its close analog ALLO-2 could inhibit Smo agonist Hh-Ag 1.5-induced luciferase expression in TM3-Gli-Luc cells. The potency of ALLO-1 did not change when either low dose or high dose of Hh-Ag 1.5 was used, in contrast to other known Smo antagonists that are strong SAG or Hh-Ag 1.5 competitors. Moreover, it was found that in contrast to GDC-0449, both ALLO-1 and ALLO-2 inhibited wild-type and the D477G mutant with only around2-fold shift in IC50, indicating that the D477G mutation did not significantly interfere with the binding of ALLO-1 and ALLO-2 to Smo. In addition, ALLO-1 as well as ALLO-2 were able to inhibit both wild-type and D473H mutant human SMO with similar potencies [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Tao, H. ,Jin, Q.,koo, D.I., et al. Small molecule antagonists in distinct binding modes inhibit drug-resistant mutant of smoothened. Chemistry & Biology 18, 432-437 (2011).
| Cas No. | 37468-32-9 | SDF | |
| 化学名 | 3-(4-chlorophenyl)-5-methyl-1-(phenylmethyl)-2,4-imidazolidinedione | ||
| Canonical SMILES | O=C1N(C2=CC=C(Cl)C=C2)C(N(CC3=CC=CC=C3)C1C)=O | ||
| 分子式 | C17H15ClN2O2 | 分子量 | 314.8 |
| 溶解度 | ≤20mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 3.1766 mL | 15.8831 mL | 31.7662 mL |
| 5 mM | 0.6353 mL | 3.1766 mL | 6.3532 mL |
| 10 mM | 0.3177 mL | 1.5883 mL | 3.1766 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet