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  4. Legubicin

Legubicin  (Synonyms: Doxorubicin-LNAA-Boc)

Cat. No.: HY-176806 Purity: 98.01%
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Legubicin (Doxorubicin-LNAA-Boc) is a novel conjugate of Doxorubicin (HY-15142A) and a Legumain-cleavable peptide linker. Legubicin is activated by Legumain to release leucine-doxorubicin while sparing normal tissues. Legubicin inhibits tumor cell growth and reduces DNA binding in non-legumain expressing cells. Legubicin completely arrests tumor growth in mice bearing CT26 tumors. Legubicin can be used for the study of colon carcinoma (CRC).

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

Legubicin

Legubicin Chemical Structure

CAS No. : 606967-53-7

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Description

Legubicin (Doxorubicin-LNAA-Boc) is a novel conjugate of Doxorubicin (HY-15142A) and a Legumain-cleavable peptide linker. Legubicin is activated by Legumain to release leucine-doxorubicin while sparing normal tissues. Legubicin inhibits tumor cell growth and reduces DNA binding in non-legumain expressing cells. Legubicin completely arrests tumor growth in mice bearing CT26 tumors. Legubicin can be used for the study of colon carcinoma (CRC)[1].

In Vivo

Legubicin (9.05 μmol/kg, i.v., single dose) enhances doxorubicin exposure in tumors and reduces it in heart/kidney in HT1080 tumor-bearing nude mice[1].
Legubicin (i.v., single dose, 56-day observation) shows higher MTD than conventional Doxorubicin (HY-15142A) in female SD rats and in beagle dogs, with milder toxicity signs[1].
Legubicin (5-25 mg/kg, i.v., once weekly, 4 weeks) induces dose-dependent toxicity in SD rats[1].
Legubicin (3/1.5-20/10 mg/kg, i.v., once weekly, 4 weeks) causes 80% mortality at 20/10 mg/kg in beagle dogs[1].
Legubicin (5-50 mg/kg, i.p., 2-day intervals, 3 times) completely arrests tumor growth without evident toxicity in Balb/C mice bearing CT26 tumors or WEHI nude mice bearing legumain293[2].

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

1013.05

Formula

C48H64N6O18
CAS No.
Appearance

Solid

Color

Orange to red

SMILES

OC1=C2C(C(C3=C(OC)C=CC=C3C2=O)=O)=C(O)C([C@H]4O[C@@H]5C[C@@H]([C@@H]([C@@H](O5)C)O)NC([C@H](CC(C)C)NC([C@H](CC(N)=O)NC([C@H](C)NC([C@H](C)NC(OC(C)(C)C)=O)=O)=O)=O)=O)=C1C[C@](O)(C4)C(CO)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (98.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9871 mL 4.9356 mL 9.8712 mL
5 mM 0.1974 mL 0.9871 mL 1.9742 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9871 mL 4.9356 mL 9.8712 mL 24.6780 mL
5 mM 0.1974 mL 0.9871 mL 1.9742 mL 4.9356 mL
10 mM 0.0987 mL 0.4936 mL 0.9871 mL 2.4678 mL
15 mM 0.0658 mL 0.3290 mL 0.6581 mL 1.6452 mL
20 mM 0.0494 mL 0.2468 mL 0.4936 mL 1.2339 mL
25 mM 0.0395 mL 0.1974 mL 0.3948 mL 0.9871 mL
30 mM 0.0329 mL 0.1645 mL 0.3290 mL 0.8226 mL
40 mM 0.0247 mL 0.1234 mL 0.2468 mL 0.6169 mL
50 mM 0.0197 mL 0.0987 mL 0.1974 mL 0.4936 mL
60 mM 0.0165 mL 0.0823 mL 0.1645 mL 0.4113 mL
80 mM 0.0123 mL 0.0617 mL 0.1234 mL 0.3085 mL
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Legubicin Related Classifications

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:

Legubicin606967-53-7Doxorubicin-LNAA-BocDrug DerivativeDrug derivativeInhibitorinhibitorinhibit

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