country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-119143

Copy Link Print Information

CB 3703

CB 3703 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR). CB 3703 has an IC₅₀ of 0.25 μM against rat TS, a K_i of 0.47 μM against mouse TS, an IC₅₀ of 6.8 nM against rat DHFR, and a K_i of 0.6 pM against mouse DHFR. CB 3703 is transported via the reduced folate pathway, has a short plasma half-life, and can prolong the survival of tumor-bearing mice. CB 3703 can be used in the research of L1210 ascites tumors.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 32093-09-7
Formel: C₂₂H₂₄N₆O₅
Molecular Weight:452.46

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

CB 3703 Chemical Structure

CAS. Nr.: 32093-09-7

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
L1210	IC50	0.019 μM	Growth inhibition against mouse L1210 cells assessed as reduction in cell count after 48 hr incubation. Growth inhibition against mouse L1210 cells assessed as reduction in cell count after 48 hr incubation.	0014296480902145

In Vitro

CB 3703 (6.8 nM-100 μM) potently inhibits rat liver DHFR (I₅₀=6.8 nM) and Yoshida ascites sarcoma TS (I₅₀=0.25 μM), and weakly inhibits other folate metabolizing enzymes at 100 μM^[1].
CB 3703 potently inhibits purified L1210 cell DHFR (K_i=0.6 pM, competitive) and purified L1210 cell TS (K_i=0.47 μM, non-competitive), and weakly inhibits rat liver methionine synthetase (K_i=0.36 mM)^[1].
CB 3703 (50 nM; 48 hr) toxicity to L1210 cells is partially reversed by thymidine or folinic acid alone, improved by their combination, and fully reversed only by thymidine plus hypoxanthine^[1].
CB 3703 (0.019 μM; 48 hr) inhibits L1210 cell growth with an I₅₀ of 0.019 μM^[1].
CB 3703 (2-40 μM; 20 min) competes with methotrexate for uptake into L1210 cells, and weakly competes with folic acid, suggesting shared transport pathways^[1].
CB 3703 (4 μM; 0-40 min) accumulates to ~10-fold higher intracellular levels than methotrexate in L1210 cells over 40 minutes, does not plateau within this time, and does not use the folic acid transport pathway^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

L1210 cells
Concentration:

0.019 μM
Incubation Time:

48 hr
Result:

Reduced L1210 cell count to 50% of control levels after 48 hr incubation at 0.019 μM.

Parmacokinetics

Species	Dose	Route	T_1/2	Plasma Concentration
Mice^[1]	10 mg/kg	i.p.	1.54 h	0.05 μM

In Vivo

CB 3703 (1-8 mg/kg; i.p.; single dose) delivers a 64% increase in median survival time at a single 2 mg/kg i.p. dose in (DBA2×C57B1)F₁ mice bearing L1210 ascites leukaemia^[1].
CB 3703 (1-8 mg/kg; i.p.; single dose) has an LD₅₀ between 2 mg/kg and 4 mg/kg in healthy female (DBA2×C57B1)F₁ mice following a single i.p. dose^[1].
CB 3703 (10 mg/kg; i.p.; single dose) exhibits a plasma half-life of 1.54 hours in healthy female (DBA2×C57B1)F₁ mice following a single 10 mg/kg i.p. dose, with barely detectable levels at 24 hours^[1].

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

Animal Model:

(DBA2×C57B1)F₁ hybrid (9-12-week-old female; L1210 leukaemia ascites model, injected i.p. with 5×10⁴ tumour cells 3 days prior to treatment)^[1]
Dosage:

1 mg/kg; 2 mg/kg; 4 mg/kg; 8 mg/kg
Administration:

i.p.; single dose
Result:

Produced a 36% increase in median survival time (from 14 days in untreated controls to 19 days).
Produced a 64% increase in median survival time (to 23 days).
Caused 3/5 tumour-bearing mice to die from toxicity before 10 days.
Caused all 5 tumour-bearing mice to die from toxicity before 10 days.

Animal Model:

(DBA2×C57B1)F₁ hybrid (9-12-week-old female; healthy, non-tumour bearing)^[1]
Dosage:

1 mg/kg; 2 mg/kg; 4 mg/kg; 8 mg/kg
Administration:

i.p.; single dose
Result:

Caused 5/11 mice to die from toxicity.
Caused 1/10 mice to die from toxicity.
Caused all 10 mice to die from toxicity.
Caused all 10 mice to die from toxicity.
Resulted in an LD₅₀ between 2 mg/kg and 4 mg/kg.

Animal Model:

(DBA2×C57B1)F₁ hybrid (9-12-week-old female; healthy, non-tumour bearing)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; single dose
Result:

Exhibited exponential plasma level decay over the first 8 hours with a half-life of 1.54 hours.
Reached barely detectable plasma levels of approximately 0.05 μM at 24 hours.

Chemical Information

CAS. Nr. 32093-09-7
Molecular Weight 452.46
Formel C₂₂H₂₄N₆O₅
SMILES

O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(NCC2=C(C)C3=C(N)N=C(N)N=C3C=C2)C=C1)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Calvert A H, et al. Quinazoline antifolates with dual biochemical loci of action. Biochemical and biological studies directed towards overcoming methotrexate resistance[J]. European Journal of Cancer (1965), 1980, 16(5): 713-722.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen