2. MAPK/ERK Pathway
  3. MAP4K
  4. HDM2004

HDM2004 是一种选择性的、具有口服活性的、可穿透血脑屏障的 HPK1 抑制剂，其 IC50 为 1.89 nM。HDM2004 对结肠癌具有抗癌活性。HDM2004 在同源小鼠模型中与抗 PD-L1 联用表现出协同活性。HDM2004 可用于结肠癌的研究。

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HDM2004

HDM2004 Chemical Structure

CAS No. : 2953016-30-1

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HDM2004 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer[1].

IC50 & Target[1]

HPK1

1.89 nM (IC50)

体外研究
(In Vitro)

HDM2004 可强效抑制重组 HPK1，其 IC50 为 1.89 nM，且对同源性较高的激酶 GLK 具有 31.88 倍的选择性 (GLK IC50 = 60.29 nM)[1]。
HDM2004 可增强经抗 CD3/抗 CD28 刺激的人外周血单个核细胞 (PBMC) 中 IL-2 的分泌，其 EC50 为 38.9 nM[1]。
HDM2004 在小鼠 (t1/2 > 300 min) 和人源 (t1/2 > 300 min) 肝微粒体中表现出极佳的稳定性[1]。
HDM2004 (1 μM) 表现出中等程度的激酶组选择性，可强效脱靶抑制 ROCK1 (抑制率 94.04%，IC50 = 230.0 nM)、VEGFR2 (抑制率 91.39%，IC50 = 116.7 nM) 和 LCK (抑制率 78.25%，IC50 = 300.1 nM)；在其余 44 个与安全性相关的靶点上未观察到显著抑制作用[1]。

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

HDM2004 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 AUC0-24 AUC0-t AUC0-∞ CL Vss Bioavailability MRTlast AUC0-last
Mice[1] 2 mg/kg i.v. / / 1.25 h / / 762 ng·h/mL 42.9 mL/min/kg 4.63 L/kg / / /
Rat[1] 10 mg/kg p.o. 486 ng/mL 2.00 h / / / 1968 ng·h/mL / / 52.0 % / /
Rat[1] 1 mg/kg i.v. / / 8.00 h / / 445 ng·h/mL 25.8 mL/min/kg 14.2 L/kg / / /
Rat[1] 5 mg/kg p.o. 83.5 ng/mL 7.33 h / / / 1130 ng·h/mL / / 55.4 % / /
Monkey[1] 1 mg/kg i.v. / / 2.14 h / / 413 ng·h/mL 41.5 mL/min/kg 7.48 L/kg / / /
Monkey[1] 20 mg/kg p.o. 306 ng/mL 11.02 h 11.02 h / / 8011 ng·h/mL / / 101 % / /
Monkey[1] 60 mg/kg p.o. 537 ng/mL 15.32 h 15.32 h / / 29254 ng·h/mL / / 78.7 % / /
Mice[1] 40 mg/kg p.o. 1693 ng/mL 4.00 h 3.67 h 16949 ng·h/mL 17455 ng·h/mL 17483 ng·h/mL / / / / /
Mice[1] 60 mg/kg p.o. 2070 ng/mL 6.00 h 3.94 h 32076 ng·h/mL 33657 ng·h/mL 33667 ng·h/mL / / / / /
Mice[1] 80 mg/kg p.o. 2333 ng/mL 6.00 h 4.52 h 35831 ng·h/mL 39755 ng·h/mL 39843 ng·h/mL / / / / /
Mice[1] 100 mg/kg p.o. 2687 ng/mL 4.00 h 9.82 h 35378 ng·h/mL 42725 ng·h/mL 44111 ng·h/mL / / / / /
Rat[1] 50 mg/kg p.o. 1076 (Plasma) ng/mL 8 (Plasma) h / / / / / / / 10.64 (Plasma) h 17554 (Plasma) ng·h/mL
体内研究
(In Vivo)

HDM2004 (口服；每日 1 次；连续 2 周；剂量 20-60 mg/kg) 在 MC38 结肠癌同源小鼠模型中呈现剂量依赖性抗肿瘤活性[1]。
HDM2004 (口服，每日 1 次，连续 2 周，剂量 20-60 mg/kg) 在 MC38 结肠癌同源小鼠模型中与抗小鼠 PD-L1 联用时表现出协同抗肿瘤活性，其中 60 mg/kg 口服每日剂量联合抗小鼠 PD-L1 时的最大 TGI 率为 77.05%[1]。

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

Animal Model: C57BL/6J (female, 6-8 weeks old, inoculated subcutaneously with MC38 colon carcinoma cells)[1]
Dosage: 20 mg/kg; 40 mg/kg; 60 mg/kg
Administration: p.o.; QD; 2 weeks
Result: Reduced mean tumor volume to 1745.74 ± 293.04 mm3 and achieved a TGI rate of 14.25% at 20 mg/kg on Day 20.
Reduced mean tumor volume to 1218.76 ± 228.78 mm3 and achieved a TGI rate of 40.07% at 40 mg/kg on Day 20.
Reduced mean tumor volume to 973.24 ± 103.47 mm3 and achieved a TGI rate of 52.10% at 60 mg/kg on Day 20.
Caused no significant body weight loss in treated mice.
Animal Model: C57BL/6J (female, 6-8 weeks old, inoculated subcutaneously with MC38 colon carcinoma cells)[1]
Dosage: 20 mg/kg (in combination with anti-mouse PD-L1); 40 mg/kg (in combination with anti-mouse PD-L1); 60 mg/kg (in combination with anti-mouse PD-L1)
Administration: p.o.; QD; 2 weeks
Result: Reduced mean tumor volume to 760.85 ± 160.55 mm3 and achieved a TGI rate of 62.62% at 20 mg/kg in combination with anti-mouse PD-L1 on Day 20.
Reduced mean tumor volume to 537.55 ± 70.74 mm3 and achieved a TGI rate of 73.56% at 40 mg/kg in combination with anti-mouse PD-L1 on Day 20.
Reduced mean tumor volume to 467.12 ± 105.04 mm3 and achieved a TGI rate of 77.05% at 60 mg/kg in combination with anti-mouse PD-L1 on Day 20.
Caused no significant body weight loss in treated mice.
分子量

485.62

Formula

C28H35N7O
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

HDM2004 相关分类

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  • 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:

HDM20042953016-30-1HDM 2004HDM-2004MAP4KMAPK Kinase Kinase KinaseGLKcytochrome P450 enzymesyngeneic mouse modelshuman PBMCsPD-L1 blockadeHPK1SLP-76human liver microsomesmc38 colon carcinomaJurkat cellsInhibitorinhibitorinhibit

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