化合物 MKC3946|TQ0101|TargetMol

MKC3946
1093119-54-0

￥558 1mg 起订

￥1650 5mg 起订

￥2710 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 MKC3946

英文名称：: MKC3946

CAS号：: 1093119-54-0

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.65%

产品类别：: 抑制剂

货号：: TQ0101

Product Introduction

Bioactivity

名称	MKC3946
描述	MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
细胞实验	For each assay, the various numbers of cells (1,000 for cell proliferation and 10,000 for cell viability assays) are seeded in 96-well plates, followed by either vehicle (DMSO) or increasing concentrations of the drug. For detection of relative numbers of living cells, 10 μL of MTT (5 mg/mL) is added to each well, placed in an incubator for four hours, followed by centrifugation (1,000 rpm, 5 min); 100 μL of supernatant media from each well are carefully removed and 100 μL of SDS buffer (20% in water) is added to dissolve the crystals. Results are further read on the spectrophotometer machine at 570 nM wavelength. Half maximal inhibitory concentration (IC50) is calculated using the GraphPad Prism 5. A synergy of combination of two drugs is determined using the CalcuSyn software. The extent of drug interaction between the two drugs is determined using the combination index (CI) for mutually exclusive drugs. Different CI values are obtained when solving the equation for different concentrations of drugs. A CI of 1 indicates an additive effect, whereas a CI of <1denotes synergy. All experiments are repeated at least three times [1].
动物实验	CB17 SCID mice (48-54 days old) are injected subcutaneously with 1×10^7 RPMI 8226 cells mixed with Matrigel on day 0, and receive treatment for 21 days starting on day1. Mice are assigned into 4 groups (n=8): daily intraperitoneal injections of 100 mg/kg MKC-3946; intravenous injections of 0.15 mg/kg bortezomib twice a week; a combination of MKC-3946 intraperitoneally with bortezomib intravenously; and 10% HPBCD intraperitoneally with normal saline intravenously as vehicle control. Tumor volume is calculated from caliper measurements every 3 to 4 days; mice are killed when tumors reached 1.5 cm in length. Survival is evaluated from the first day of treatment until death [3].
体外活性	MKC-3946通过阻断XBP1 mRNA剪接，并对AML细胞展现细胞毒性。MKC-3946抑制由tunicamycin (TM)在NB4细胞(B)及患者AML样本[1]中诱导的XBP1S表达。MKC-3946阻止因突变前胰岛素产生造成的内质网应激响应中XBP1 mRNA的剪接[2]。作为IRE1α核糖核酸酶领域抑制剂，MKC-3946阻断XBP1 mRNA剪接，在多发性骨髓瘤（MM）细胞中触发适度的生长抑制。MKC-3946以剂量依赖方式抑制由Tm诱导的XBP1s表达，但不影响IRE1α的磷酸化。MKC-3946阻断XBP1剪接，并增强由bortezomib或17-AAG诱导的细胞毒性。MKC-3946（10μM）增强了由bortezomib或17-AAG引起的内质网应激介导的凋亡，并即使在BMSCs或外源性IL-6存在的情况下，也增强了内质网应激剂的细胞毒性[3]。
体内活性	MKC-3946（100 mg/kg，i.p.）在体内ER应激模型中抑制XBP1剪接，与显著的MM细胞生长抑制相关，无论是单独使用还是与博腾珠单抗联用。MKC-3946显著降低了治疗组相比对照组的MM肿瘤生长。通过MKC-3946抑制XBP1剪接与体内MM生长减少相关，无论是单独使用还是与博腾珠单抗联用[3]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 30 mg/mL (78.85 mM)
关键字	Inositol requiring enzyme 1 \| inhibit \| IRE1 \| Inhibitor \| MKC3946 \| MKC-3946 \| MKC 3946
相关产品	D-F07 \| 4μ8C \| GSK2850163 (S enantiomer) \| Sunitinib Malate \| 6-Bromo-2-hydroxy-3-methoxybenzaldehyde \| Sunitinib \| APY29 \| Toyocamycin \| B I09 \| IXA4 \| MKC8866 \| GSK2850163
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 抗癌化合物库 \| 已知活性化合物库 \| 细胞周期化合物库 \| 激酶抑制剂库 \| 临床前化合物库 \| 血液病分子库 \| 内质网应激化合物库

MKC3946|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务