2. Membrane Transporter/Ion Channel
  3. Sec61
  4. KZR-261

KZR-261 is a Sec61 translocase inhibitor. KZR-261 binds directly to the Sec61 channel, thereby inhibiting the biosynthesis of certain Sec61 substrate proteins, including oncogenic factors. KZR-261 activates the endoplasmic reticulum stress response. KZR-261 exhibits broad in vitro anticancer activity. KZR-261 shows antitumor efficacy in mouse models of cancer. KZR-261 can be used for the research of multiple myeloma, colorectal cancer, small cell lung cancer, pancreatic cancer, prostate cancer, non-Hodgkin's lymphoma, and mantle cell lymphoma.

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

KZR-261

KZR-261 Chemical Structure

CAS No. : 2376747-46-3

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Based on 1 publication(s) in Google Scholar

KZR-261 Related Antibodies

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Description

KZR-261 is a Sec61 translocase inhibitor. KZR-261 binds directly to the Sec61 channel, thereby inhibiting the biosynthesis of certain Sec61 substrate proteins, including oncogenic factors. KZR-261 activates the endoplasmic reticulum stress response. KZR-261 exhibits broad in vitro anticancer activity. KZR-261 shows antitumor efficacy in mouse models of cancer. KZR-261 can be used for the research of multiple myeloma, colorectal cancer, small cell lung cancer, pancreatic cancer, prostate cancer, non-Hodgkin's lymphoma, and mantle cell lymphoma[1].

IC50 & Target

Caspase 3

 

Caspase-7

 

In Vitro

KZR-261 (0.1-1000 nM; 1 h pre-incubation, 24 h total) reduces the cell surface expression levels of certain Sec61 substrate proteins in stimulated human peripheral blood mononuclear cells (PBMCs) in a dose-dependent manner, with the highest potency observed for CD62L (IC50 = 4 nM) and IL-7R (IC50 = 12 nM)[1].
KZR-261 (250 nM; 24 h) selectively inhibits a small subset of Sec61 substrate proteins (1.7-1.8% of detected substrates) in multiple myeloma cell lines, and even fewer substrates (0.5% of detected substrates) in primary human PBMCs, with a preference for secretory and type I/II transmembrane substrates[1].

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

KZR-261 Related Antibodies
In Vivo

KZR-261 (7.5 mg/kg; intravenous injection; once weekly; for 3-8 weeks) achieves 100% tumor growth inhibition in the H929 multiple myeloma xenograft model, with minimal effects on body weight[1].
KZR-261 (intravenous injection, once weekly for 3-8 weeks at 5-10 mg/kg) induces tumor growth inhibition in the HT-29 colorectal cancer xenograft model[1].
KZR-261 (administered intravenously; once weekly; for 3-8 weeks at 5 mg/kg) induces tumor growth inhibition in H82 small cell lung cancer xenografts[1].
KZR-261 (intravenous injection, once weekly for 3-8 weeks at 10 mg/kg) induces tumor growth inhibition in BxPC-3 pancreatic cancer xenografts[1].
KZR-261 (15 mg/kg; intravenous injection; once weekly; for 3-8 weeks) induces tumor growth inhibition in 22Rv1 prostate cancer xenografts[1].
KZR-261 (10 mg/kg; intravenous injection; once weekly; for 3-8 weeks) induces tumor growth inhibition in the RL non-Hodgkin's lymphoma xenograft model[1].
KZR-261 (20 mg/kg; intravenous injection; once weekly; for 3-8 weeks) induces tumor growth inhibition in Mino mantle cell lymphoma xenografts[1].
KZR-261 (10 mg/kg; intravenous injection; once weekly for 3 consecutive weeks) achieves 77% tumor growth inhibition in the MC38-hPD-L1 colorectal cancer xenograft model of hPD-1 gene-knockin mice, and combination with Pembrolizumab (HY-P9902) leads to complete tumor regression[1].

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

Animal Model: beige/nude/xid (female, 5-7 weeks old, implanted with 3×107 H929 cells)[1]
Dosage: 7.5 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Achieved 100% tumor growth inhibition (TGI) with minimal effects on body weight.
Animal Model: athymic nude (female, 5-7 weeks old, implanted with 5×106 HT-29 cells)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Resulted in statistically significant tumor growth inhibition relative to vehicle control.
Animal Model: athymic nude (female, 5-7 weeks old, implanted with 5×106 H82 cells)[1]
Dosage: 5 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Resulted in statistically significant tumor growth inhibition relative to vehicle control.
Animal Model: athymic nude (female, 5-7 weeks old, implanted with 5×106 BxPC-3 cells)[1]
Dosage: 10 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Resulted in statistically significant tumor growth inhibition relative to vehicle control.
Animal Model: athymic nude (male, 5-7 weeks old, implanted with 1×107 22Rv1 cells)[1]
Dosage: 15 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Achieved a greater level of tumor control than etoposide (dosed per established protocols), with statistically significant tumor growth inhibition relative to vehicle control.
Animal Model: athymic nude (female, 5-7 weeks old, implanted with 1×107 RL cells)[1]
Dosage: 10 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Resulted in statistically significant tumor growth inhibition relative to vehicle control.
Animal Model: athymic nude (female, 5-7 weeks old, implanted with 5×106 Mino cells)[1]
Dosage: 20 mg/kg
Administration: i.v.; once weekly; 3-8 weeks
Result: Resulted in statistically significant tumor growth inhibition relative to vehicle control.
Animal Model: hPD-1 plus C57BL/6 (Biocytogen) (female, implanted with 5×105 MC38-hPD-L1 cells)[1]
Dosage: 10 mg/kg/2.5 mg/kg (pembrolizumab)
Administration: i.v.; once weekly; 3 weeks
Result: Achieved 77% tumor growth inhibition (TGI) by study day 27; tumor recovery was observed 1 week after the final dose, resulting in 53% TGI at that time point.
Achieved complete tumor regression (104% TGI) by study day 27; no tumors were observed within 7 days of the last dose, with complete response in 5 of 10 mice.
Molecular Weight

765.06

Formula

C38H61FN6O5S2
CAS No.
SMILES

O=S(N1CCCN(CCCN(C[C@H](C1)C)S(N2C[C@H](N([C@@H](C2)C)C3=CC(OC)=CC(F)=C3)C)(=O)=O)CC4CCCCC4)(C5=CC=C(C=C5)N(C)C)=O
Shipping

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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KZR-261 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:

KZR-2612376747-46-3KZR261KZR 261Sec61Sec61 complex, SecY, Sec61 channelSec61 translocase inhibitormalignant diseasesmultiple myelomacolorectal cancersmall cell lung cancerpancreatic cancerprostate cancernon-Hodgkin's lymphomaand mantle cell lymphomabeige/nude/xid miceathymic nude micehPD-1 plus C57BL/6 miceInhibitorinhibitorinhibit

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