Topo I Inhibitor

Topo I Inhibitors (142):

Cat. No.	Product Name	Effect	Purity

HY-15142

Doxorubicin hydrochloride	Inhibitor	99.90%
Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride; ADR), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC₅₀s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy.

HY-13631D

DXd	Inhibitor	99.30%
DXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC₅₀ of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

HY-13704

SN-38	Inhibitor	99.94%
SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC₅₀s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).

HY-16562

Irinotecan	Inhibitor	99.97%
Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.

HY-16560

Camptothecin	Inhibitor	99.77%
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.

HY-13631U

Exatecan hydrochloride	Inhibitor
Exatecan (DX-8951) hydrochloride is a DNA topoisomerase I inhibitor, with an IC₅₀ of 2.2 μM (0.975 μg/mL), and can be used in cancer research.

HY-171946

TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT	Inhibitor
TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT is a drug-linker conjugate for ADC. TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT consists of a topoisomerase 1 inhibitor (Topi MF-6) (HY-175203) and a cleavable linker (Maleimide-Ph(3,5-F)-PEG4-Val-Ala) (HY-175218). TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT can be used for synthesis of ADCs.

HY-N2062

10-Nitrocamptothecin	Inhibitor
10-Nitrocamptothecin is a topoisomerase I inhibitor with an IC₅₀ of 0.64 μM. 10-Nitrocamptothecin interferes with the formation of cleavable complexes, thereby inhibiting the activity of Topoisomerase I. 10-Nitrocamptothecin is applicable for cancer research.

HY-141598

Datopotamab deruxtecan (solution)	Inhibitor	99.98%
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 K_d of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer.

HY-13768A

Topotecan hydrochloride	Inhibitor	99.89%
Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

HY-16562A

Irinotecan hydrochloride	Inhibitor	99.89%
Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.

HY-P3371

Ifinatamab deruxtecan	Inhibitor	99.29%
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects

HY-10529

Betulinic acid	Inhibitor	99.88%
Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.

HY-13555

β-Lapachone	Inhibitor	99.96%
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

HY-13631DS

DXd-d₅	Inhibitor	99.02%
DXd-d₅ is a deuterium labeled DXd. DXd is a potent DNA topoisomerase I inhibitor, with an IC₅₀ of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .

HY-171945

Telisotuzumab Adizutecan	Inhibitor	99.63%
Telisotuzumab Adizutecan (ABBV-400) is an anti-c-Met antibody-drug conjugate (ADC). Telisotuzumab Adizutecan is composed of the humanized anti-c-Met antibody Telisotuzumab (HY-P99391) and the topoisomerase 1 inhibitor (7-MAD-MDCPT) (HY-132162). Telisotuzumab Adizutecan exhibits significant anti-tumor activity against advanced solid tumors such as colorectal cancer, gastric cancer, and non-small cell lung cancer.

HY-16700

PNU-159682	Inhibitor	98.50%
PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.

HY-16568

Irinotecan hydrochloride trihydrate	Inhibitor	99.89%
Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.

HY-N2306

Aclacinomycin A	Inhibitor	99.30%
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.

HY-13566A

Belotecan hydrochloride	Inhibitor	99.97%
Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.

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