1. Cell Cycle/DNA Damage Others
  2. Topoisomerase Drug Intermediate
  3. β-Glu-PAB(CH2NH2)-Exatecan

β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers.

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

β-Glu-PAB(CH2NH2)-Exatecan Chemical Structure

β-Glu-PAB(CH2NH2)-Exatecan Chemical Structure

CAS No. : 3025108-11-3

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Description

β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers[1].

IC50 & Target

Topoisomerase

 

Molecular Weight

790.74

Formula

C39H39FN4O13

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NCC(C=C1COC(N[C@@H]2C3=C4C(C(N5C4)=CC([C@](O)(C(OC6)=O)CC)=C6C5=O)=NC7=CC(F)=C(C)C(CC2)=C73)=O)=C(C=C1)O[C@@H]8O[C@@H]([C@H]([C@@H]([C@H]8O)O)O)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (126.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2646 mL 6.3232 mL 12.6464 mL
5 mM 0.2529 mL 1.2646 mL 2.5293 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 (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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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 (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 1.2646 mL 6.3232 mL 12.6464 mL 31.6160 mL
5 mM 0.2529 mL 1.2646 mL 2.5293 mL 6.3232 mL
10 mM 0.1265 mL 0.6323 mL 1.2646 mL 3.1616 mL
15 mM 0.0843 mL 0.4215 mL 0.8431 mL 2.1077 mL
20 mM 0.0632 mL 0.3162 mL 0.6323 mL 1.5808 mL
25 mM 0.0506 mL 0.2529 mL 0.5059 mL 1.2646 mL
30 mM 0.0422 mL 0.2108 mL 0.4215 mL 1.0539 mL
40 mM 0.0316 mL 0.1581 mL 0.3162 mL 0.7904 mL
50 mM 0.0253 mL 0.1265 mL 0.2529 mL 0.6323 mL
60 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5269 mL
80 mM 0.0158 mL 0.0790 mL 0.1581 mL 0.3952 mL
100 mM 0.0126 mL 0.0632 mL 0.1265 mL 0.3162 mL
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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.

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Product Name:
β-Glu-PAB(CH2NH2)-Exatecan
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HY-173703
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