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My CartCAS：1229705-06-9
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1229705-06-9 |
| Name | Idasanutlin |
| Molecular Formula | C31H29Cl2F2N3O4 |
| Molecular Weight | 616.48 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD26142931 |
| SMILES | O=C(O)C1=CC(OC)=C(NC([C@H]2[C@H](C3=C(F)C(Cl)=CC=C3)[C@](C4=CC=C(Cl)C=C4F)(C#N)[C@H](CC(C)(C)C)N2)=O)C=C1 |
| Target Point | MDM-2 |
| Passage | Apoptosis |
| Background | Idasanutlin is a potent and selective MDM2 antagonist capable of inhibiting p53-MDM2 binding. |
| Biological Activity | Idasanutlin 是一种有效，选择性的 MDM2 拮抗剂，能够抑制 p53-MDM2 的结合，IC50 值为 6 nM。[1-2] |
| IC50 | 6nM(p53-MDM2)[1] |
| In Vitro | Idasanutlin抑制细胞增殖，IC50为30 nM，诱导剂量依赖性p53稳定，细胞周期停滞，以及表达野生型p53的癌细胞中的细胞凋亡[1]。 Idasanutlin(300 nM或1.8μM)诱导SJSA骨肉瘤细胞凋亡[2]。 |
| In Vivo | Idasanutlin(25 mg/kg po)在小鼠SJSA人骨肉瘤异种移植模型中导致肿瘤生长抑制和消退[1]。 Idasanutlin在SJSA异种移植模型中诱导细胞凋亡和抗增殖[2]。 |
| Cell Experiment | 通过四唑染料测定评估细胞增殖。从浓度的对数与抑制百分比的图的线性回归确定细胞增殖的50％抑制(IC 50)或90％抑制(IC 90)的浓度。 |
| Animal Experiment | 在10至12周龄时，给小鼠植入悬浮在无酚基质胶和PBS中的人SJSA骨肉瘤细胞(ATCC)的1：1混合物。将小鼠植入右侧，浓度为5×106个细胞，总体积为0.2mL。在大约第10天，根据肿瘤体积随机化动物，使得10只随机小鼠的所有组具有相似的起始平均肿瘤体积100至250mm 3。 Idasanutlin(RG7388)作为无定形固体分散体微量沉淀物粉末施用，其含有30％药物物质和70％乙酸琥珀酸羟丙基甲基纤维素聚合物，其在施用前立即重构为Klucel/Tween中的悬浮液，并且在给药后丢弃剩余的悬浮液。 |
| Data Literature Source | [1]. Ding Q，et al. Discovery of RG7388，a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013 Jul 25;56(14):5979-83. [2]. Higgins B，et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clin Cancer Res. 2014，20(14)，3742-3752 |
| Unit | Bottle |
| Specification | 2mg 5mg 10mg |
是一种有效，选择性的 MDM2 拮抗剂，能够抑制 p53-MDM2 的结合。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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