2. Apoptosis Cell Cycle/DNA Damage
  3. Thymidylate Synthase DNA/RNA Synthesis
  4. OSI-7904L

OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a Ki of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma.

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

OSI-7904L

OSI-7904L Chemical Structure

CAS No. : 139987-54-5

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.

OSI-7904L Related Antibodies

Top Publications Citing Use of Products

View All DNA/RNA Synthesis Isoform Specific Products:

View All Isoforms
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a Ki of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma[1][2].

In Vitro

OSI-7904L potently inhibits the growth of all tested human cell lines with sub-1 nM IC50, with thymidine alone reversing this effect; murine cell lines are 80-1300-fold less sensitive than human cell lines[2].

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

OSI-7904L Related Antibodies
Parmacokinetics
Species Dose Route AUC0-∞ AUC0-last CL Cmax MRT0-∞ Vss
Mice[1] 1.0 mg/kg i.v. 133 μg·h/mL 118 μg·h/mL 7.69 mL/h/kg 13.9 μg/mL 10.8 h 81.4 mL/kg
Mice[1] 10.0 mg/kg i.v. 2530 μg·h/mL 2530 μg·h/mL 3.97 mL/h/kg 154 μg/mL 17.0 h 67.1 mL/kg
Mice[1] 50.0 mg/kg i.v. 16900 μg·h/mL 16800 μg·h/mL 2.97 mL/h/kg 797 μg/mL 25.8 h 76.4 mL/kg
In Vivo

OSI-7904L (7.5 mg/kg; i.v.; every other day; 14 days) achieves 97.5% TGI, 83% tumor regression in HCT-8 TK-/- tumor-bearing Nu/Nu mice[1].
OSI-7904L (7.5-25 mg/kg; i.v.; three distinct schedules: daily × 5 for 2 weeks, on days 1,3,5 for 2 weeks, or on days 1 and 8) achieves 95-97% TGI, 86-88% tumor regression, and 1 durable cure per group in HCT-8 TK-/- tumor-bearing Nu/Nu mice[1].
OSI-7904L (5-25 mg/kg; i.v.; on days 1 and 8) produces a dose-dependent response in HCT-8 TK-/- tumor-bearing Nu/Nu mice, with 80-99% TGI, 0-100% tumor regression, and 0-4 durable cures at day 60[1].

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

Animal Model: Nu/Nu nude (female, 18-25 g)[1]
Dosage: 7.5 mg/kg (total dose 52.5 mg/kg)
Administration: i.v.; every other day; 14 days
Result: Achieved 83% tumor regression, a log cell kill (LCK) index of 4.6, and 97.5% tumor growth inhibition (TGI) on day 23.
Produced transient, reversible body weight loss that never exceeded 10%.
Animal Model: Nu/Nu nude (female, 18-25 g)[1]
Dosage: 7.5 mg/kg (daily on days 1-5 for 2 consecutive weeks); 15 mg/kg (on days 1, 3, 5 for 2 consecutive weeks); 25 mg/kg (on days 1 and 8)
Administration: i.v.; daily on days 1-5 for 2 consecutive weeks; i.v.; on days 1, 3, 5 for 2 consecutive weeks; i.v.; on days 1 and 8
Result: Demonstrated 96% TGI, 88% tumor regression on day 22, LCK of 3.9, and 1/8 durable cures with the 7.5 mg/kg schedule.
Demonstrated 95% TGI, 86% tumor regression on day 22, LCK of 3.2, and 1/8 durable cures with the 15 mg/kg schedule.
Demonstrated 97% TGI, 88% tumor regression on day 22, LCK of 4.2, and 1/8 durable cures with the 25 mg/kg schedule.
Animal Model: Nu/Nu nude (female, 18-25 g)[1]
Dosage: 5 mg/kg; 10 mg/kg; 15 mg/kg; 20 mg/kg; 25 mg/kg
Administration: i.v.; on days 1 and 8
Result: Produced 80% TGI on day 26, 0% tumor regression, and 0 cures at 5 mg/kg.
Produced 92% TGI on day 26, 58% tumor regression, and 0 cures at 10 mg/kg.
Produced 95% TGI on day 26, 65% tumor regression, and 1 cure at 15 mg/kg.
Produced 97% TGI on day 26, 100% tumor regression, and 2 cures at 20 mg/kg.
Produced 99% TGI on day 26, 100% tumor regression, and 4 cures at 25 mg/kg.
Caused no appreciable body weight effects in any dose group.
Clinical Trial
Molecular Weight

500.50

Formula

C27H24N4O6
CAS No.
SMILES

O=C1C2=C3C(C=CC(CNC4=CC=C(C(N(C5)[C@H](C(O)=O)CCC(O)=O)=O)C5=C4)=C3)=CC=C2NC(C)=N1
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.

OSI-7904L 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:

OSI-7904L139987-54-5GW1843 1843U89 OSI-7904GW 1843GW-1843OSI7904OSI 7904OSI-7904Thymidylate SynthaseDNA/RNA Synthesisreduced folate carriercolon adenocarcinomaHCT-8 TK-/-murine L1210 cellsmouse xenograft modelshuman cellsMOLT-4 cellsthymidylate synthasemicehog liver folylpolyglutamate synthetaseInhibitorinhibitorinhibit

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:
OSI-7904L
Cat. No.:
HY-10823
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.