2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs DNA/RNA Synthesis Apoptosis
  4. LC-1-40

LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).

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LC-1-40 Chemical Structure

LC-1-40 Chemical Structure

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LC-1-40 Related Antibodies

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Description

LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research[1]. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).

IC50 & Target

DC50: 0.97 nM (NUDT1)[1].
In Vitro

LC-1-40 (0.1, 1, 10, 50, 100 µM; 0.5, 1, 2, 4, 6 h) induces a dose- and time-dependent NUDT1 degradation in SHEP MYCN-ER cells[1].

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

LC-1-40 Related Antibodies

Western Blot Analysis[1]

Cell Line: SHEP MYCN-ER cells
Concentration: 0.1, 1, 10, 50, 100 µM
Incubation Time: 0.5, 1, 2, 4, 6 h
Result: Induced NUDT1 degradation in a dose- and time-dependent manner.
In Vivo

LC-1-40 (30 mg/kg; i.p.; once daily for 15 days) selectively impeds the growth of MYCN-amplified T409 tumors in mice[1].
1.19 Pharmacokinetic Parameters of LC-1-40 in male C57BL/6 mice[1].

IV (5 mg/kg) IP (30 mg/kg) PO (30 mg/kg)
T1/2 (h) 6.34 42.7 7.13
Tmax (h) 0.08 3.33 3.33
Cmax (ng/mL) 4373 3080 1923
AUCInf (h*ng/mL) 32571 59799 25063
CL (mL/min/kg) 2.57 - -
Vss (mL/kg) 1.2 - -
F (%) - 32.7 14.2

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

Animal Model: T409 xenografts model[1].
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; once daily for 15 days
Result: Inhibited the growth of NUDT1-related tumor.
Animal Model: Male C57BL/6 mice[1].
Dosage: 50 mg/kg, 30 mg/kg
Administration: Intravenous/Intraperitoneal/Oral; single dose
Result: Exhibited an oral bioavailability of 14.2%, nominating it as a promising lead for further optimization
Molecular Weight

844.96

Formula

C49H48N8O6
SMILES

O=C1CCC(C(N1)=O)N2C(C3=C(C2=O)C=C(C=C3)N4CCN(CC4)CC5CCN(CC5)C(C6=CC=C(C=C6)C7=CC=C8N=CC(C(NC9CC9)=O)=C(C8=C7)NC%10=CC=CC=C%10)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LC-1-40 Related Classifications

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

LC-1-40PROTACsDNA/RNA SynthesisApoptosiscancertumorCRISPR-Cas9MYCNOX4PLK1KellySF188Inhibitorinhibitorinhibit

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