VVD-118313
目录号 : GC67867VVD-118313 (compound 5a) 是一个有效的选择性 JAK1 抑制剂。VVD-118313 靶向异构体限制性变构半胱氨酸 (C817)，阻断 JAK1 依赖的反式磷酸化和细胞因子信号。VVD-118313 可用于癌症的研究。
Cas No.:2875046-27-6
Sample solution is provided at 25 µL, 10mM.
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VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1].
VVD-118313 (compound 5a; 0.01-10 μM; 3 h; primary human PBMCs) inhibits JAK1 by engagement of C817 and JAK2 by engagement of C838. VVD-118313 inhibits cysteine reactivity in a dose-dependent manner[1].
VVD-118313 (2 µM, 2h) blocks IFNα-simulated STAT1 and IL-6-stimulated STAT3 phosphorylation in WT- or C810A-JAK1-expressing 22Rv1 cells. VVD-118313 also blocks the constitutive phosphorylation of WT- and C810A-JAK1[1].
VVD-118313 (0.01-10 μM) selectively inhibits JAK1 signaling in primary human immune cells. VVD-118313 inhibits JAK1-dependent IFNα-pSTAT1, IL-6-pSTAT3, and IL-2-pSTAT5 pathways in human PBMCs in a dose-dependent manner[1].
VVD-118313 (0.1-0.4 μM; 24h) inhibits T-cell activation induction. VVD-118313 inhibits the activation of human T cells co-stimulated with αCD3/αCD28 by a reduction in the proportion of CD25+ T cells. VVD-118313 blocks the secretion of the Th1-polarizing cytokine IFNγ and increases the production of IL-2[1].
VVD-118313 (0.1-0.5 μM; 2h) inhibits on the production of pro-inflammatory cytokines and chemokines. VVD-118313 suppresses the induction of several pro-inflammatory chemokines, including CCL2/MCP-1, CXCL10/IP-10, and CCL4/MIP-1β[1].
Western Blot Analysis[1]
| Cell Line: | 22Rv1 cells |
| Concentration: | 0.01, 0.1, and 1 μM |
| Incubation Time: | 2 hours |
| Result: | Showed labeling of recombinant WT-JAK1 and C810A-JAK1, but not C817A-JAK1. |
Western Blot Analysis[1]
| Cell Line: | 22Rv1 cells |
| Concentration: | 2 µM |
| Incubation Time: | 2 hours |
| Result: | Inhibited WT- and C810A-JAK1 phosphorylation with even greater potency than STAT1/STAT3 phosphorylation. |
VVD-118313 (compound 5a; 25-50 mg/kg; i.h.; once; TYK2 knockout mice) inhibits JAK1 signaling in mice[1].
| Animal Model: | TYK2 knockout mice[1] |
| Dosage: | 25 and 50 mg/kg |
| Administration: | Subcutaneous injection; once |
| Result: | Revealed 75% engagement of JAK1_C816 at 25 and 50 mg/kg, while other JAK1 cysteines were unaffected in reactivity. |
[1]. Kavanagh ME, et, al. Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine. Nat Chem Biol. 2022 Sep 12.
| Cas No. | 2875046-27-6 | SDF | Download SDF |
| 分子式 | C19H22Cl2N2O3S | 分子量 | 429.36 |
| 溶解度 | 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 | 2.329 mL | 11.6452 mL | 23.2905 mL |
| 5 mM | 0.4658 mL | 2.329 mL | 4.6581 mL |
| 10 mM | 0.2329 mL | 1.1645 mL | 2.329 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet