KZR-261

Name: KZR-261
Brand: MedChemExpress
SKU: HY-176763
Rating: 4.5 (0 reviews)

Cat. No.: HY-176763 Purity: 99.39%: Data Sheet
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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 Chemical Structure

CAS No. : 2376747-46-3

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote	Estimated Time of Arrival: December 31
100 mg	Get quote	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Description

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.

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.

2376747-46-3

Appearance

Solid

Color

White to off-white

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (130.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3071 mL	6.5354 mL	13.0709 mL
5 mM	0.2614 mL	1.3071 mL	2.6142 mL
10 mM	0.1307 mL	0.6535 mL	1.3071 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.27 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.27 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.39%

Select Batch:

Data Sheet (285 KB) SDS (252 KB)

COA (261 KB) HNMR (445 KB) RP-HPLC (262 KB) LCMS (132 KB)

Handling Instructions (2659 KB)

References

[1]. Lowe E, et al. Preclinical characterization of novel multi-client inhibitors of Sec61 with broad antitumor activity. J Pharmacol Exp Ther. 2025;392(8):103634. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3071 mL	6.5354 mL	13.0709 mL	32.6772 mL
	5 mM	0.2614 mL	1.3071 mL	2.6142 mL	6.5354 mL
	10 mM	0.1307 mL	0.6535 mL	1.3071 mL	3.2677 mL
	15 mM	0.0871 mL	0.4357 mL	0.8714 mL	2.1785 mL
	20 mM	0.0654 mL	0.3268 mL	0.6535 mL	1.6339 mL
	25 mM	0.0523 mL	0.2614 mL	0.5228 mL	1.3071 mL
	30 mM	0.0436 mL	0.2178 mL	0.4357 mL	1.0892 mL
	40 mM	0.0327 mL	0.1634 mL	0.3268 mL	0.8169 mL
	50 mM	0.0261 mL	0.1307 mL	0.2614 mL	0.6535 mL
	60 mM	0.0218 mL	0.1089 mL	0.2178 mL	0.5446 mL
	80 mM	0.0163 mL	0.0817 mL	0.1634 mL	0.4085 mL
	100 mM	0.0131 mL	0.0654 mL	0.1307 mL	0.3268 mL

KZR-261 Related Classifications

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.

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KZR-261

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Complete Stock Solution Preparation Table

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