SBI-0206965

Name: SBI-0206965
Brand: MedChemExpress
SKU: HY-16966
Rating: 5.0 (25 reviews)

Cat. No.: HY-16966 Purity: 99.39%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2.

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

SBI-0206965 Chemical Structure

CAS No. : 1884220-36-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 83	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 83	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 385	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 605	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 25 publication(s) in Google Scholar

24 Publications Citing Use of MCE SBI-0206965

: SBI-0206965 purchased from MedChemExpress. Usage Cited in: BioMedicine. 2018 Aug;34:85-93. [Abstract]; A498 and ACHN cells are cultured in starvation medium (EBSS) with SBI-0206965 (0 μM, 5 μM, 10 μM, and 20 μM) for 24 h. Phosphorylation of Ser108 of the AMPK β1 subunit, cleavage of PARP and Caspase 8, and levels of LC3B and p62 are measured by western blot analysis.

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ULK1 ULK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2^[1].

IC₅₀ & Target^[1]

ULK1

108 nM (IC₅₀)

ULK2

711 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	6.78 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
HL-60	IC₅₀	18.92 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MCF7	IC₅₀	26.17 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MDA-MB-468	IC₅₀	18.38 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MDA-MB-468	IC₅₀	2.1 μM Compound: 1; SBI-0206965	Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 33200929]
U-937	IC₅₀	25.12 μM Compound: SBI-0206963; SBI-0206965	Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]

In Vitro

SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation^[1].
SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis^[1].

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

Apoptosis Analysis^[1]

Cell Line:	A498 and ACHN cells (starvation medium (EBSS) treatment)
Concentration:	5, 10 ,20 μM
Incubation Time:	24 hours
Result:	Induced significant levels of apoptosis.

Western Blot Analysis^[1]

Cell Line:	A498 and ACHN cells (EBSS treatment)
Concentration:	5, 10, 20 μM
Incubation Time:	24 hours
Result:	Attenuated the phosphorylation of Ser108 of the AMPK β1 subunit and increased the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluated by analysis of LC3B and p62.

In Vivo

SBI-0206965 (50?mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours^[1].

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

Animal Model:	Six-week-old male BALB/c nude mice (A498 xenograft tumours)^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; once every three days for 37 days
Result:	Significantly suppressed tumour growth.

Molecular Weight

489.32

Formula

C₂₁H₂₁BrN₄O₅

CAS No.

1884220-36-3

Appearance

Solid

Color

White to off-white

SMILES

CNC(C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br)=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 (204.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0437 mL	10.2183 mL	20.4365 mL
5 mM	0.4087 mL	2.0437 mL	4.0873 mL
10 mM	0.2044 mL	1.0218 mL	2.0437 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 (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.11 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 (281 KB) SDS (252 KB)

COA (252 KB) LCMS (95 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[1]. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell RenalCarcinoma and the Antitumor Effects of SBI-0206965. EBioMedicine. 2018 Aug;34:85-93. [Content Brief]

[2]. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-97. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0437 mL	10.2183 mL	20.4365 mL	51.0913 mL
	5 mM	0.4087 mL	2.0437 mL	4.0873 mL	10.2183 mL
	10 mM	0.2044 mL	1.0218 mL	2.0437 mL	5.1091 mL
	15 mM	0.1362 mL	0.6812 mL	1.3624 mL	3.4061 mL
	20 mM	0.1022 mL	0.5109 mL	1.0218 mL	2.5546 mL
	25 mM	0.0817 mL	0.4087 mL	0.8175 mL	2.0437 mL
	30 mM	0.0681 mL	0.3406 mL	0.6812 mL	1.7030 mL
	40 mM	0.0511 mL	0.2555 mL	0.5109 mL	1.2773 mL
	50 mM	0.0409 mL	0.2044 mL	0.4087 mL	1.0218 mL
	60 mM	0.0341 mL	0.1703 mL	0.3406 mL	0.8515 mL
	80 mM	0.0255 mL	0.1277 mL	0.2555 mL	0.6386 mL
	100 mM	0.0204 mL	0.1022 mL	0.2044 mL	0.5109 mL

SBI-0206965 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.

Keywords:

SBI-02069651884220-36-3SBI0206965SBI 0206965ULKAutophagyApoptosisUnc-51 like kinaseInhibitorinhibitorinhibit

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SBI-0206965

Customer Review

SBI-0206965 Related Antibodies

24 Publications Citing Use of MCE SBI-0206965

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•Related Screening Libraries:

•Related Small Molecules:

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View All ULK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

SBI-0206965 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SBI-0206965 Related Classifications

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