2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. TL033

TL033 is a drug-Linker conjugates for ADC. TL033 contains a linker and bioactive small molecule toxins. TL033 can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer.

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TL033

TL033 Chemical Structure

CAS No. : 2356230-22-1

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Based on 1 publication(s) in Google Scholar

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Description

TL033 is a drug-Linker conjugates for ADC. TL033 contains a linker and bioactive small molecule toxins. TL033 can conjugate with Sacituzumab antibody (anti Trop-2) for synthesizing BT001021. BT001021 has anti-cancer activities against various cancers, such as breast cancer, non-small cell lung cancer (NSCLC), gastric cancer[1].

In Vitro

BT001021 (3 days) shows killing effects (EC50: 13.15 nM) on HCC1806 cells (breast cancer cell line)[1].

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

TL033 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCC1806 (Trop-2 positive cell line)
Concentration: 0-50 nM approximately
Incubation Time: 3 days
Result: Showed cytoxicity with an EC50 value of 13.15 nM.
In Vivo

BT001021 (intravenous injection, 3 mg/kg, twice a week for a total of 6 times) inhibits the tumor growth of xenograft model mice of NCI-N87 gastric cancer, and tumor regression occurres at the end of administration[1].
BT001021 (intravenous injection, 10 mg/kg for a single dose) shows significant tumor tissue targetability and good pharmacokinetic properties[1].

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

Animal Model: Xenograft of a human gastric cancer cell line NCI-N87[1]
Dosage: 3 mg/kg
Administration: Intravenous injection, twice a week for a total of 6 times.
Result: Significantly inhibited the tumor growth (114.61%) without significant toxicity.
Animal Model: Xenograft of a human triple negative breast cancer cell line HCC1806[1];
Xenograft model mice of HCC827 non-small cell lung cancer (NSCLC)[1].
Dosage: 10 mg/kg
Administration: Intravenous injection, twice a week for a total of 6 times.
Result: Effectively inhibited the tumor growth (54.93% for breast cancer, 108.7% for NSCLC).
Animal Model: Xenograft of a human gastric cancer cell line NCI-N87 (pharmacokinetic assay)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection for a single dose
Result: Pharmacokinetic parameters of BT001021 in tumors and serum.
Tumor Serum
Cmax (ng/mL) 7.82 11.7/sub>
Tmax (h) 8.0 1.0
T1/2 (h) 93.14 44.35
Molecular Weight

1630.83

Formula

C76H103N13O23S2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N2C(C3=NC4=CC=CC=C4C(CCN(C(C)C)S(C)(=O)=O)=C3C2)=CC5=C1COC([C@@]5(CC)OC(OCC6=CC=C(C=C6)NC([C@H](CCCCN)NC(COCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCN7C=C(N=N7)CNC(CCCC#CC8=CN=C(S(C)(=O)=O)N=C8)=O)=O)=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

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

Purity & Documentation
References
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TL033 Related Classifications

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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:

TL0332356230-22-1TL 033TL-033Drug-Linker Conjugates for ADCCancerbreast cancerNSCLCgastric cancer TL033BT001021SacituzumabtoxinNCI-N87HCC827HCC1806Inhibitorinhibitorinhibit

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