2. MAPK/ERK Pathway Immunology/Inflammation
  3. MAP4K Interleukin Related
  4. HPK1-IN-69

HPK1-IN-69 是一种具有口服活性的 HPK1 抑制剂，IC50 为 1.7 nM。HPK1-IN-69 可抑制 HPK1 介导的 TCR 信号通路，降低 SLP76 的磷酸化水平，促进 IL-2 的释放。HPK1-IN-69 在小鼠模型中表现出体内抗肿瘤活性。HPK1-IN-69 可用于结直肠癌和 MC38 同源肿瘤的研究。

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HPK1-IN-69

HPK1-IN-69 Chemical Structure

CAS No. : 3095423-83-6

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HPK1-IN-69 相关抗体

Top Publications Citing Use of Products

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HPK1-IN-69 is an orally active HPK1 inhibitor with an IC50 of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors[1].

IC50 & Target[1]

HPK1

 

IL-2

 

体外研究
(In Vitro)

HPK1-IN-69 (compound 53) (0-300 nM; 2 h pre-incubation) 可剂量依赖性地抑制 Jurkat T 细胞中 CD3/CD28 诱导的 SLP76 磷酸化，其 pSLP76 的 IC50 为 23.1 nM[1]。
HPK1-IN-69 (0-1000 nM; 1 h pre-incubation) 可剂量依赖性地增强 Jurkat T 细胞 (EC50 = 29.9 nM) 和 hPBMC 中 CD3/CD28 诱导的 IL-2 释放，且可逆转 PGE2 介导的 IL-2 抑制作用[1]。
HPK1-IN-69 (0-60 min) 在小鼠和人肝微粒体中表现出良好的代谢稳定性，半衰期超过 30 min[1]。
HPK1-IN-69 对人 CYP 同工酶表现出弱抑制作用，其 IC50 值范围为 6.1 μM 至 >50 μM，提示其在 CYP 相互作用方面具有特定的安全窗[1]。
HPK1-IN-69 对 hERG 通道的抑制活性相对较低，其 IC50 为 7.92 μM，提示其心脏毒性风险较低[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HPK1-IN-69 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 0, 1, 3, 10, 30, 100, 300 nM
Incubation Time: 2 h (pre-incubation prior to 10 min CD3/CD28 stimulation)
Result: Dose-dependently inhibited SLP76 phosphorylation in Jurkat cells, with a cellular IC50 of 23.1 nM for pSLP76 inhibition.
药代动力学
(Parmacokinetics)
Species Dose Route Vss_obs CL_obs AUC0-t T1/2 Cmax Tmax AUC0-∞ Bioavailability
Rat[1] 1.0 mg/kg i.v. 88.8 mL/kg 287.6 mL/min/kg 41.8 ng·h/mL 3.9 h / / / /
Rat[1] 10.0 mg/kg i.g. / / / / 5.8 ng/mL 6.7 h 27.9 ng·h/mL 6.7 %
体内研究
(In Vivo)

HPK1-IN-69 (15-30 mg/kg；腹腔注射；每日 2 次；连续 17 天) 在 CT26 结直肠癌小鼠模型中展现出剂量依赖性的抗肿瘤功效[1]。
HPK1-IN-69 (15-60 mg/kg；腹腔注射/口服；每日 2 次；连续 21 天) 在 MC38 结直肠癌小鼠模型中展现出强效抗肿瘤功效，60 mg/kg 口服剂量下的肿瘤生长抑制率 (TGI) 达 64%；且与抗 PD-1 抗体联用具有协同活性，可实现 77% 的 TGI[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (female, 18-22 g, 4-5 weeks old, subcutaneous inoculation of CT26 cells)[1]
Dosage: 15 mg/kg; 30 mg/kg; 30 mg/kg
Administration: i.p.; twice daily; 17 days
Result: Achieved a tumor growth inhibition (TGI) rate of 36% at 15 mg/kg.
Achieved a TGI of 62% at 30 mg/kg, with significantly reduced tumor weight relative to the model group.
Achieved a TGI of 75% when combined with anti-PD-1 antibody.
Enhanced CD8+ T-cell infiltration into tumor tissue in a dose-dependent manner.
Caused no significant body weight loss or major organ damage.
分子量

416.48

Formula

C22H24N8O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HPK1-IN-69 相关分类

  • 摩尔计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HPK1-IN-693095423-83-6MAP4KInterleukin RelatedMAPK Kinase Kinase KinaseILMC38 syngeneic tumorIL-2mouse modelscolorectal cancerhPBMCsJurkat T cellsTCR signalingCLK1HPK1SLP76Inhibitorinhibitorinhibit

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目录号：
HY-182238
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