Navtemadlin AMG 232; KRT-232|cas:1352066-68-2|西域试剂

Navtemadlin AMG 232; KRT-232,99.43%

产品编号：Bellancom-12296| CAS NO：1352066-68-2| 分子式：C₂₈H₃₅Cl₂NO₅S| 分子量：568.55

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货号	价格	库存与货期
Bellancom-12296	￥1700.00	杭州北京（现货）
Bellancom-12296	￥2600.00	杭州北京（现货）
Bellancom-12296	￥5750.00	杭州北京（现货）
Bellancom-12296	￥9500.00	杭州北京（现货）
Bellancom-12296	￥15000.00	杭州北京（现货）

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Navtemadlin AMG 232; KRT-232

产品介绍

Navtemadlin (AMG 232) 是一种有效，选择性，可口服的 p53-MDM2 相互作用抑制剂，IC₅₀ 值为 0.6 nM，与 MDM2 结合的 K_d 为 0.045 nM。

生物活性

Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM.

体外研究

Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines.
Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC₅₀=10 nM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347 and A427 cells.
Concentration:	0-10 μM.
Incubation Time:	72 hours.
Result:	Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN). Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.

体内研究
(In Vivo)

Navtemadlin (AMG 232) (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo.
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice.
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo.
Navtemadlin causes a dose-dependent tumor growth inhibition with an ED₅₀ of 16 mg/kg.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice (n=10/group) based cancer models.
Dosage:	10, 25, 75 mg/kg.
Administration:	Once daily by oral gavage.
Result:	Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED₅₀ of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice (n=10/group) based cancer models.
Dosage:	10, 25, 75 mg/kg.
Administration:	Once daily by oral gavage.
Result:	Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED₅₀ of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice (n=10/group) based cancer models.
Dosage:	10, 25, 75 mg/kg.
Administration:	Once daily by oral gavage.
Result:	Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED₅₀ of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (87.94 mM)

H₂O : ≥ 0.1 mg/mL (0.18 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7589 mL	8.7943 mL	17.5886 mL
5 mM	0.3518 mL	1.7589 mL	3.5177 mL
10 mM	0.1759 mL	0.8794 mL	1.7589 mL

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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 50% PEG300 50% saline
Solubility: 10 mg/mL (17.59 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution
5.

请依序添加每种溶剂： PBS
Solubility: 1.5 mg/mL (2.64 mM); Clear solution; Need ultrasonic