HPK1-IN-55

CAS: 3048537-58-9 F: C30H34N8O3 W: 554.64

HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC5

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Bioactivity	HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of 637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects[1].
Invitro	HPK1-IN-55 (0.5-10000 nM, 5 h) 在 human PBMCs 中显示出酶抑制作用 (IC50<0.51 nM) 和细胞效力 (EC50 = 43.3 nM) [1]。HPK1-IN-55 (0.001-100 nM) 在 human PBMCs 中刺激 IL-2 和 IFN-γ 的释放，EC50 值分别为 38.8 和 49.2 nM[1]。HPK1-IN-55 (0.00457-10 μM, 72 h) 在人体免疫 T 细胞中低、中、高浓度下均能促进 T 细胞增殖[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HPK1-IN-55 相关抗体: Cell Proliferation Assay [1] Cell Line:
In Vivo	HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) 作为单一疗法具有良好的抗肿瘤作用，当与 anti-PD-1 联合使用时，在 CT26 模型中显示出相加作用，在 MC38 模型中表现出协同作用[1]。HPK1-IN-55 (1 mg/kg, i.v., 2 mg/kg, p.o.) 在猴子体内表现出中等清除率 (Clp = 11.41 mL/min/kg)，良好的口服暴露 (DNAUC (0−24 h) =560.5 h•ng/mL) 和生物利用度 (F % = 42.0)[1]。HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) 在 CT26 模型中表现出良好的靶向参与[1]。 HPK1-In-55的体内药代动力学指标
CAS	3048537-58-9
Formula	C30H34N8O3
Molar Mass	554.64
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Peng J, et.al. Discovery of Pyridine-2-Carboxamides Derivatives as Potent and Selective HPK1 Inhibitors for the Treatment of Cancer. J Med Chem. 2024 Dec 12;67(23):21520-21544.

E3 Ligase Ligand-linker Conjugate 157