GDC-0575 (ARRY-575, RG7741)
(Synonyms: (R)-N-(4-(3-氨基哌啶-1-基)-5-溴-1H-吡咯并[2,3-B]吡啶-3-基)环丙烷甲酰胺,ARRY-575; RG7741) 目录号 : GC32885
A Chk1 inhibitor
Cas No.:1196541-47-5
Sample solution is provided at 25 µL, 10mM.
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GDC-0575 is an inhibitor of checkpoint kinase 1 (Chk1; IC50 = 1.2 nM).1 It is greater than 30-fold selective for Chk1 over a panel of more than 450 wild-type and mutant kinases. GDC-0575 (500 nM) enhances apoptosis induced by cytarabine in HL-60, KG-1, U937, and ML-1 human acute myeloid leukemia (AML) cells. It nearly completely eliminates tumor burden in AML patient-derived xenograft (PDX) mouse models when administered at a dose of 7.5 mg/kg in combination with cytarabine.
1.Di Tullio, A., Rouault-Pierre, K., Abarrategi, A., et al.The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemiaNat. Commun.8(1)1679(2017)
Cell experiment: | AML cell lines are seeded at 1×104 cells/well in 96-well plates in triplicate, and subjected to different treatment conditions. After 24 h of incubation with GDC-0575, cell proliferation is measured with the XTT Cell Proliferation Kit II[3]. |
Animal experiment: | Mice[1]Female nude BALB/c mice are injected with 2-3×106 melanoma cells in Matrigel by subcutaneous injection on the hind flank. Once tumors reach approximately 100 mm3, mice are treated with GDC-0575 (25 mg/kg, 50 mg/kg) or vehicle (0.5% w/v methylcellulose and 0.2%v/v Tween 80) by oral gavage for 3 cycles where one cycle is three consecutive days of treatment followed by four rest days. Tumor size is measured three times per week using calipers. Mice are sacrificed at up to 6 weeks after terminating the treatment or when tumor size measured >1 cm3[1]. |
References: [1]. Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Mar 13. doi: 10.1158/1078-0432.CCR-17-2701. | |
| Cas No. | 1196541-47-5 | SDF | |
| 别名 | (R)-N-(4-(3-氨基哌啶-1-基)-5-溴-1H-吡咯并[2,3-B]吡啶-3-基)环丙烷甲酰胺,ARRY-575; RG7741 | ||
| Canonical SMILES | O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32 | ||
| 分子式 | C16H20BrN5O | 分子量 | 378.27 |
| 溶解度 | DMSO : ≥ 50 mg/mL (132.18 mM) | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6436 mL | 13.2181 mL | 26.4361 mL |
| 5 mM | 0.5287 mL | 2.6436 mL | 5.2872 mL |
| 10 mM | 0.2644 mL | 1.3218 mL | 2.6436 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet