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

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.

For research use only. We do not sell to patients.

HDM2004

HDM2004 Chemical Structure

CAS No. : 2953016-30-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

HDM2004 Related Antibodies

Top Publications Citing Use of Products

View All MAP4K Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

In Vitro

HDM2004 potently inhibits recombinant HPK1 with an IC50 of 1.89 nM, and exhibits 31.88-fold selectivity over the highly homologous kinase GLK (GLK IC50 = 60.29 nM)[1].
HDM2004 enhances IL-2 secretion in human peripheral blood mononuclear cells (PBMCs) stimulated with anti-CD3/anti-CD28, with an EC50 of 38.9 nM[1].
HDM2004 exhibits excellent stability in mouse (t1/2 > 300 min) and human (t1/2 > 300 min) liver microsomes[1].
HDM2004 (1 μM) exhibits moderate kinome selectivity, with potent off-target inhibition of ROCK1 (94.04% inhibition, IC50 = 230.0 nM), VEGFR2 (91.39% inhibition, IC50 = 116.7 nM) and LCK (78.25% inhibition, IC50 = 300.1 nM); no significant inhibitory effect is observed on the remaining 44 safety-related targets[1].

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

HDM2004 Related Antibodies
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
In Vivo

HDM2004 (20-60 mg/kg; p.o.; QD; 2 weeks) exhibits dose-dependent antitumor activity in the MC38 colon carcinoma syngeneic mouse model, with a maximum TGI rate of 52.10% at the 60 mg/kg oral daily dose[1].
HDM2004 (20-60 mg/kg; p.o.; QD; 2 weeks) exhibits synergistic antitumor activity when combined with anti-mouse PD-L1 in the MC38 colon carcinoma syngeneic mouse model, with a maximum TGI rate of 77.05% at the 60 mg/kg oral daily dose plus anti-mouse PD-L1[1].

MedChemExpress (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.
Molecular Weight

485.62

Formula

C28H35N7O
CAS No.
SMILES

CCN(CC1)CCC1N(N=C2)C=C2C3=CNC4=C3N=C(C5=CC=C(N6C[C@@H](C)O[C@H](C)C6)C=C5)C=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

HDM2004 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
HDM2004
Cat. No.:
HY-181932
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.