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MK-8776

SCH 900776

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂，IC50为3 nM，比作用于Chk2选择性高50倍,是高效口服生物相容性的Chk1抑制剂,对Chk2和CDK2的IC50则分别为1500 nM和160 nM。

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生物活性

SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).
体外研究
体内研究

4% DMSO+30% propylene glycol
激酶实验
细胞实验
动物实验

~50 mg/kg 腹腔内注射
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Guzi TJ, et al. Mol Cancer Ther, 2011, 10(4), 591-602.

分子式 C15H18BrN7	分子量 376.25	CAS号 891494-63-6	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO 4 mg/mL	Water <1 mg/mL	Ethanol <1 mg/mL

体内溶解度

NCT Number	Conditions	Interventions	Sponsor/Collaborators	Phases	Start Date	Last Updated
NCT00907517	Myelogenous Leukemia, Acute\|Leukemia, Lymphocytic, Acute\|Leukemia, Lymphoblastic, Acute, Philadelphia-Positive\|Myelogenous Leukemia, Chronic, Aggressive Phase	Drug: MK-8776\|Drug: Cytarabine	Merck Sharp & Dohme Corp.	Phase 1	2009-07-01	2016-11-30
NCT01870596	Adult Acute Megakaryoblastic Leukemia\|Adult Acute Monoblastic Leukemia\|Adult Acute Monocytic Leukemia\|Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11\|Adult Acute Myeloid Leukemia With Maturation\|Adult Acute Myeloid Leukemia With Minimal Differentiation\|Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11\|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22); RUNX1-RUNX1T1\|Adult Acute Myeloid Leukemia With t(9;11)(p22;q23); MLLT3-MLL\|Adult Acute Myeloid Leukemia Without Maturation\|Adult Acute Myelomonocytic Leukemia\|Adult Erythroleukemia\|Adult Pure Erythroid Leukemia\|Alkylating Agent-Related Acute Myeloid Leukemia\|Recurrent Adult Acute Myeloid Leukemia	Drug: Cytarabine\|Drug: CHK1 Inhibitor SCH 900776\|Other: Laboratory Biomarker Analysis	National Cancer Institute (NCI)	Phase 2	2013-05-01	2016-07-20
NCT00779584	Hodgkin Disease\|Lymphoma, Non-Hodgkin\|Neoplasms	Drug: SCH 900776\|Drug: Gemcitabine	Merck Sharp & Dohme Corp.	Phase 1	2008-10-01	2015-02-25
NCT01521299	Advanced Solid Tumors	Drug: Hydroxyurea	Dartmouth-Hitchcock Medical Center	Phase 1	2012-03-01	2012-08-24

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。