A-770041
目录号 : GC35213
A LCK kinase inhibitor
Cas No.:869748-10-7
Sample solution is provided at 25 µL, 10mM.
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A-770041 is an inhibitor of LCK kinase (IC50 = 0.147 ?M).1 It is selective for LCK over other Src family tyrosine kinases including Src, Fyn, Fgr, HCK, and Tie2 (IC50s = 9.05, 44.1, 14.1, 1.22, and >50 ?M, respectively). A-770041 induces dephosphorylation of LCK by SHP-1, inactivating LCK, in IgE/antigen-stimulated bone marrow-derived mast cells (BMMCs).2 It inhibits IL-2 production induced by an anti-CD3 antibody and phorbol 12-myristate 13-acetate in isolated human whole blood (EC50 = 80 nM) and by concanavalin A in rats.3 A-770041 (10 mg/kg) prevents acute rejection and increases graft survival in a rat model of heterotopic heart transplantation. It also inhibits the growth of CTV-1 human acute myeloid leukemia cells (IC50 = 224 nM) and sensitizes U2OSMR and KHOSR2 multidrug resistant human osteosarcoma cells to paclitaxel and doxorubicin .4,5
1.Burchat, A., Borhani, D.W., Calderwood, D.J., et al.Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejectionBioorg. Med. Chem. Lett.16(1)118-122(2006) 2.Chang, H.W., Kanegasaki, S., Jin, F., et al.A common signaling pathway leading to degranulation in mast cells and its regulation by CCR1-ligandAllergy75(6)1371-1381(2020) 3.Stachlewitz, R.F., Hart, M.A., Bettencourt, B., et al.A-770041, a novel and selective small-molecule inhibitor of Lck, prevents heart allograft rejectionJ. Pharmacol. Exp. Ther.315(1)36-41(2005) 4.Li, L., Cui, Y., Shen, J., et al.Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1Leuk. Res.7812-20(2019) 5.Duan, Z., Zhang, J., Ye, S., et al.A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cellsBMC Cancer14681(2014)
| Cas No. | 869748-10-7 | SDF | |
| Canonical SMILES | NC1=C2C(N([C@@H]3CC[C@@H](N4CCN(C(C)=O)CC4)CC3)N=C2C5=CC=C(NC(C6=CC7=C(C=CC=C7)N6C)=O)C(OC)=C5)=NC=N1 | ||
| 分子式 | C34H39N9O3 | 分子量 | 621.73 |
| 溶解度 | DMSO: ≥ 100 mg/mL (160.84 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 | 1.6084 mL | 8.0421 mL | 16.0842 mL |
| 5 mM | 0.3217 mL | 1.6084 mL | 3.2168 mL |
| 10 mM | 0.1608 mL | 0.8042 mL | 1.6084 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet