规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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靶点 |
Cereblon
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体外研究 (In Vitro) |
埃拉吉度胺诱导的 GSPT1 耗竭会导致急性髓性白血病 (AML) 细胞凋亡快速发生,从而降低 35 种不同 AML 样本的大规模原发性患者异种移植中的白血病干细胞 (LSC) 和白血病植入。在 AML 原始细胞和 LSC 中,埃拉吉多胺的活性由多层信号网络和通路介导[1]。
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参考文献 |
分子式 |
C22H18CLF2N3O4
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分子量 |
461.8458
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精确质量 |
461.10
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元素分析 |
C, 57.21; H, 3.93; Cl, 7.68; F, 8.23; N, 9.10; O, 13.86
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CAS号 |
1860875-51-9
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外观&性状 |
Solid powder
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SMILES |
O=C(NCC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2)=O)C=C1)C(F)(C4=CC=C(Cl)C=C4)F
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InChi Key |
PWBHUSLMHZLGRN-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H18ClF2N3O4/c23-15-4-2-14(3-5-15)22(24,25)21(32)26-10-12-1-6-16-13(9-12)11-28(20(16)31)17-7-8-18(29)27-19(17)30/h1-6,9,17H,7-8,10-11H2,(H,26,32)(H,27,29,30)
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化学名 |
2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide
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别名 |
CC-90009; CC 90009; CC90009
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO : 92~100 mg/mL ( 199.19~216.52 mM )
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1652 mL | 10.8260 mL | 21.6521 mL | |
5 mM | 0.4330 mL | 2.1652 mL | 4.3304 mL | |
10 mM | 0.2165 mL | 1.0826 mL | 2.1652 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04297124 | Completed | Drug: CC-90009 Radiation: [14C] |
Healthy Volunteer | Celgene | March 11, 2020 | Phase 1 |
NCT02848001 | Active, not recruiting | Drug: CC-90009 | Leukemia, Myeloid, Acute Myelodysplastic Syndromes |
Celgene | November 14, 2016 | Phase 1 |
NCT04336982 | Active, not recruiting | Drug: CC-90009 Drug: Venetoclax Drug: Azacitidine |
Leukemia, Myeloid, Acute | Celgene | August 5, 2020 | Phase 1 Phase 2 |
CC-90009, a GSPT1-selective cereblon modulator, induces cereblon-and GSPT1-dependent anti-AML activity. [1].Blood. 2021 Feb 4;137(5):661-677. td> |
Identification of genes and pathways modulating the response to CC-90009 via CRIPSR/Cas9 screen. [1].Blood. 2021 Feb 4;137(5):661-677. td> |
Regulation of CRBN splicing and CC-90009 response by the ILF2 and ILF3 complex. [1].Blood. 2021 Feb 4;137(5):661-677. td> |