2. Immunology/Inflammation
  3. FLAP
  4. MSC778

MSC778 是一种具有选择性和口服活性的 flap 核酸内切酶 1 (FEN1) 抑制剂，其 IC50 为 3 nM，KD 为 2.9 nM。MSC778 对 EXO1、GEN1 和 XPG 的选择性分别为 145 倍、516 倍和 65 倍。MSC778 可选择性杀伤 BRCA2 缺陷型细胞，并增强 Niraparib (HY-10619) 在 BRCA2 KO DLD-1 小鼠异种移植瘤中诱导肿瘤停滞的活性。MSC778 可用于结直肠癌的研究。

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MSC778

MSC778 Chemical Structure

CAS No. : 3098173-17-9

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MSC778 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer[1].

体外研究
(In Vitro)

MSC778 (7 days) 选择性杀死 BRCA2 敲除的 DLD-1 细胞，EC50值为 210 nM (表观值)，蛋白结合校正后的游离 EC50 (EC50,ub) 为 11 nM[1]。

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

MSC778 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Dog 0.2 mg/kg i.v. Cmax 1240 ng/mL
Dog 16 mg/kg p.o. Cmax 6000 ng/mL
Mice 0.2 mg/kg i.v. Cmax 2490 ng/mL
Mice 10 mg/kg p.o. Cmax 6030 ng/mL
Mice 30 mg/kg p.o. Cmax 30500 ng/mL
Rat 0.2 mg/kg i.v. Cmax 1950 ng/mL
Rat 10 mg/kg p.o. Cmax 5860 ng/mL
Dog 0.2 mg/kg i.v. AUC 2520 ng·h/mL
Dog 16 mg/kg p.o. AUC 43200 ng·h/mL
Mice 0.2 mg/kg i.v. AUC 8510 ng·h/mL
Mice 10 mg/kg p.o. AUC 56900 ng·h/mL
Mice 30 mg/kg p.o. AUC 229536 ng·h/mL
Rat 0.2 mg/kg i.v. AUC 2240 ng·h/mL
Rat 10 mg/kg p.o. AUC 27400 ng·h/mL
Dog 16 mg/kg p.o. F 21 %
Mice 10 mg/kg p.o. F 16 %
Mice 30 mg/kg p.o. F 16 %
Rat 10 mg/kg p.o. F 15 %
体内研究
(In Vivo)

MSC778 (100 mg/kg，灌胃，每天两次，持续 28 天) 增强了 Niraparib 在小鼠结直肠癌异种移植模型中诱导肿瘤停滞的活性[1]。

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

Animal Model: BRCA2 KO DLD-1 cells xenograft model established in Balb/c nude, female mice[1]
Dosage: 100 mg/kg with or without Niraparib
Administration: Oral gavage (i.g.), twice daily for 28 days
Result: Observed no tumor growth inhibition (TGI) with the single-agent treatment.
Achieved 93% TGI in the combined treatment group, resulting in tumor stasis.
No weight loss or clinical signs of toxicity.
分子量

441.86

Formula

C22H20ClN3O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MSC778 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MSC7783098173-17-9MSC 778MSC-778FLAP5-lipoxygenase-activating protein5-LO activating proteinFragment-Based Drug DiscoveryBRCA2 KO DLD-1 CellsMouse Xenograft ModelSPRPK/ADME ProfileInhibitorinhibitorinhibit

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