RBN-2397

Name: RBN-2397
Brand: MedChemExpress
SKU: HY-136174
Rating: 5.0 (17 reviews)

Cat. No.: HY-136174 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

RBN-2397 is a potent, accross species and orally active NAD⁺ competitive inhibitor of PARP7 (IC₅₀<3 nM). RBN-2397 selectively binds to PARP7 (K_d=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.

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RBN-2397 화학구조

CAS No. : 2381037-82-5

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 17 publication(s) in Google Scholar

17 Publications Citing Use of MCE RBN-2397

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PARP Isoform Specific Products:

View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[2]

PARP-7

3 nM (IC₅₀)

PARP-7

1 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
AML12	IC₅₀	>50 μM Compound: RBN-2397	Cytotoxicity against mouse AML12 cells assessed as inhibition of cell growth measured after 6 days by MTT assay Cytotoxicity against mouse AML12 cells assessed as inhibition of cell growth measured after 6 days by MTT assay	[PMID: 36576395]
AML12	IC₅₀	>50 μM Compound: RBN-2397	Antiproliferative activity against mouse AML12 cells measured after 6 days incubation by MTT assay Antiproliferative activity against mouse AML12 cells measured after 6 days incubation by MTT assay	[PMID: 38059836]
CT26	IC₅₀	12.59 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by MTT assay Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by MTT assay	[PMID: 36576395]
CT26	IC₅₀	2.31 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by CTG assay Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by CTG assay	[PMID: 38059836]
CT26	IC₅₀	5.29 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by MTT assay Antiproliferative activity against mouse CT26 cells measured after 6 days incubation by MTT assay	[PMID: 38059836]
CT26	IC₅₀	6.33 μM Compound: RBN-2397	Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 36576395]
MV4-11	IC₅₀	0.51 μM Compound: 6; RBN-2397	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay	[PMID: 38456618]
MV4-11	IC₅₀	7.97 μM Compound: 6; RBN-2397	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay	[PMID: 38456618]
NCI-H1373	IC₅₀	0.13 μM Compound: 6; RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days in presence of vorinostat by celltiter-glo luminescent assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days in presence of vorinostat by celltiter-glo luminescent assay	[PMID: 38456618]
NCI-H1373	IC₅₀	0.18 μM Compound: 6; RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by celltiter-glo luminescent assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by celltiter-glo luminescent assay	[PMID: 38456618]
NCI-H1373	IC₅₀	4.76 nM Compound: RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 36576395]
NCI-H1373	IC₅₀	40 nM Compound: RBN-2397	Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell viability incubated for 4 days by luminescence based assay Antiproliferative activity against human NCI-H1373 cells assessed as inhibition of cell viability incubated for 4 days by luminescence based assay	[PMID: 37826932]
NCI-H1373	IC₅₀	45.3 nM Compound: RBN-2397	Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay	[PMID: 38277917]
U-937	IC₅₀	0.73 μM Compound: 6; RBN-2397	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days in presence of vorinostat by celltiter-glo luminescent assay	[PMID: 38456618]
U-937	IC₅₀	20.79 μM Compound: 6; RBN-2397	Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo luminescent assay	[PMID: 38456618]

In Vitro

RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC₅₀ value of 20 nM in NCI-H1373 lung cancer cells^[2].
RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells^[2].
RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC₅₀ value of 1 nM^[2].

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

Cell Proliferation Assay^[2]

Cell Line:	NCI-H1373 lung cancer cells
Concentration:	0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time:	24 hours
Result:	Blocked cell proliferation.

Western Blot Analysis^[2]

Cell Line:	NCI-H1373 lung cancer cells
Concentration:	0.4 nM-1 μM
Incubation Time:	24 hours
Result:	Increased p-STAT1 protein expression.

In Vivo

RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice^[2].
RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg^[2].
The half-life (t_1/2) of RBN-2397 in vivo is 325 mins^[2].

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

Animal Model:	CB17 SCID mice with NCI-H1373 xenografts^[2]
Dosage:	3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; 24-32 days
Result:	Decreased tumor volume and exerted anti-tumor effects.

Clinical Trial

분자량

523.43

화학식

C₂₀H₂₃F₆N₇O₃

CAS No.

2381037-82-5

Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C(F)(F)F)=C(N[C@@H](C)COCCC(N2CCN(C3=NC=C(C(F)(F)F)C=N3)CC2)=O)C=NN1

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 200 mg/mL (382.10 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	1.9105 mL	9.5524 mL	19.1048 mL
5 mM	0.3821 mL	1.9105 mL	3.8210 mL
10 mM	0.1910 mL	0.9552 mL	1.9105 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

몰농도 계산기
농도 희석 계산기

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: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 5

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution

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.

순도&문서

Purity: 99.82%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (245 KB) HNMR (268 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency

[2]. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9105 mL	9.5524 mL	19.1048 mL	47.7619 mL
	5 mM	0.3821 mL	1.9105 mL	3.8210 mL	9.5524 mL
	10 mM	0.1910 mL	0.9552 mL	1.9105 mL	4.7762 mL
	15 mM	0.1274 mL	0.6368 mL	1.2737 mL	3.1841 mL
	20 mM	0.0955 mL	0.4776 mL	0.9552 mL	2.3881 mL
	25 mM	0.0764 mL	0.3821 mL	0.7642 mL	1.9105 mL
	30 mM	0.0637 mL	0.3184 mL	0.6368 mL	1.5921 mL
	40 mM	0.0478 mL	0.2388 mL	0.4776 mL	1.1940 mL
	50 mM	0.0382 mL	0.1910 mL	0.3821 mL	0.9552 mL
	60 mM	0.0318 mL	0.1592 mL	0.3184 mL	0.7960 mL
	80 mM	0.0239 mL	0.1194 mL	0.2388 mL	0.5970 mL
	100 mM	0.0191 mL	0.0955 mL	0.1910 mL	0.4776 mL

RBN-2397 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:

RBN-23972381037-82-5RBN2397RBN 2397PARPpoly ADP ribose polymeraseovarianadvancedmetastaticsolidtumorlungcarcinomasquamouscellNSCLCInhibitorinhibitorinhibit

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RBN-2397

고객리뷰

RBN-2397 Related Antibodies

17 Publications Citing Use of MCE RBN-2397

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PARP Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

RBN-2397 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

RBN-2397 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report