Name: RSM-932A
Brand: GlpBio
SKU: GC18847
Availability: InStock
Rating: 5 (36 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

Cell experiment [1]:
Cell lines	DLD-1, HT29, SW620 and HCT116 CRC cell lines and the non-tumourigenic CCD-841 cell line
Preparation Method	6000 cells/well were seeded into 96- well flat-bottom plates and incubated for 24 h under standard conditions. MN58b or RSM-932A (TCD-717) were added at different concentrations from stocks solutions.
Reaction Conditions	2, 3, 4 µM, 24h
Applications	RSM-932A (TCD-717; 2-4 µM; for 24 hours) promotes cell death of colon cancer cells. ChoKα specific inhibitor RSM-932A (TCD-717), has demonstrated a potent antitumoral activity both in vitro and in vivo against several tumor-derived cell line xenografts including CRC-derived cell lines.
Animal experiment [2]:
Animal models	Six-week-old nude mice
Preparation Method	Mice were s.c. inoculated at lowers flanks with 1 × 106 of HT-29 cells suspended in 100μL of serum-free DMEM media mixed (1:1) with Matrigel. Measurable subcutaneous tumors (~0.15-0.2 cm3) were randomized to the treatment and control group. Tumor growth was monitored three times per week.
Dosage form	Effective dose of RSM-932A is 7.5 mg/kg, RSM-932A was dissolved at 50 mM 100% DMSO and administrated by i.v.. The successive dilutions were done fresh every day of treatment in sterile 5% dextrose water.
Applications	This could be used to perform growth inhibition studies at the specified effective dose. No significant organ damage was observed apart from hepatotoxicity that was found in all treatments except for the less aggressive treatment with RSM-932A that showed no liver toxicity while retaining a potent antitumoral activity.
References: [1]. de la Cueva A, et al. Combined 5-FU and ChoKα inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts. PLoS One. 2013 Jun 10;8(6):e64961. [2]. Lacal JC, et al. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9.

RSM-932A is a ChoKα inhibitor with potent in vitro antiproliferative activity against a large variety of tumor-derived cell lines and in vivo antitumoral activity against human xenographs in mice. RSM-932A also shows high efficacy with low toxicity at the effective doses.^[1]

In vitro experiments indicated that RSM-932A has a potent antiproliferative activity against most tumor-derived cell lines tested, including those derived from breast, lung, colon, bladder, liver, ovary, bone, cervix, kidney, pancreas, melanoma and brain tumors, with IC50 (1.15 ± 0.14 μM) in the low, single-digit micromolar range, consistent with a cytotoxic effect.

		RSM-932A (72 h)
Type of tumor	Cell line	IC₅₀	±SD	GI₅₀	±SD	TGI	±SD	LC₅₀	±SD
Breast	MDA-MB-231	1.3	0.5	1.2	0.2	2.0	0.1	2.7	1.2
	T47D	2,2	0,9	1,3	0,8	NA	NA	>6	NA
	MDA.MB.468	2.4	1.0	1.6	0.4	3.1	1.6	>6	0.5
	SkBr-3	3.1	0.6	1.0	0.6	1.6	0.5	13.2	6.7
Lung	H510	1.4	0.3	1.0	NA	1.1	0.5	3.9	1.8
	H1299	1.9	0.1	1.0	0.0	1.9	0.7	7.4	3.0
	H460	1.9	0.5	1.0	0.0	1.7	0.6	5.2	1.3
Colon	HT-29	1.7	0.4	1.3	0.2	5.6	6.6	11.0	5.4
	HCT-116	1.8	0.3	1.0	0.3	1.7	1.0	>6	NA
	DLD-1	2.1	0.7	1.6	0.5	3.3	0.9	6.3	2.8
	SW620	2.1	0.7	1.6	0.5	3.3	0.9	6.3	2.8
Bladder	HT-1376	1.5	0.3	1.0	0.0	5.7	1.2	>6.5	NA
	TccSup	1.6	0.2	1.1	0.5	1.5	0.0	>6.5	NA
	SW780	1.6	0.4	1.4	0.3	2.3	0.5	8.2	3.1
	J82	2.3	1.3	1.6	1.2	NA	NA	5.0	2.1
Epithelial carcinoma	A431	2.2	0.1	1.5	0.5	NA	NA	3.5	0.7
Liver	Hep3B2	2.4	0.5	1.2	0.1	2.7	1.4	3.2	0.8
	HepG2	6.4	2.2	1.3	0.3	8.4	1.3	>12	NA
Ovary	OV-Car-3	3.4	0.3	1.7	0.2	2.9	0.4	5.5	0.5
	SK-OV-3	6.4	2.2	1.3	0.3	8.4	1.3	>12	NA
Bone	SAOS-2	1.3	0.1	<1.6	NA	2.2	0.7	5.1	1.5
Cervix	HeLa	1.7	0.7	1.0	NA	1.5	0.0	5.7	1.2
Kidney	769-P	1.4	0.2	1.0	0.4	2.4	1.2	>3.5	0.7
Melanoma	SKMel-28	1.3	0.3	0.5	0.0	0.4	0.1	1.5	0.4
	A-375	6.2	1.9	2.6	1.4	5.6	1.1	7.7	1.4
Pancreas	Mia.PaCa.2	2.3	0.2	1.7	0.3	3.5	0.4	5.5	1.4
Astrocytoma, gliocystoma	U-87	1.9	0.5	1.4	0.2	5.0	1.2	8.9	4.3
Control	MCF10-A	7.1	0.5	3.4	0.8	7.2	1.3	14.7	1.3

Table 1.Panel of human cancer cell lines tested with RSM-932A for 72 hours and determination of IC₅₀, GI₅₀, TGI, and LC₅₀ parameters

In vivo experiments demonstrated that RSM-932A shows no detectable toxicity in mice at highly effective doses with 77% tumor growth inhibition.^[1]

References:
[1]. Lacal JC, et al. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9.

Cas No.	850807-63-5	SDF
Synonyms	TCD-717
Chemical Name	1,1'-[[[1,1'-biphenyl]-4,4'-diyl]bis(methylene)]bis[4-[(4-chlorophenyl)methylamino]-quinolinium, dibromide
Canonical SMILES	ClC1=CC=C(N(C2=CC=[N+](CC3=CC=C(C4=CC=C(C[N+]5=C(C=CC=C6)C6=C(N(C7=CC=C(Cl)C=C7)C)C=C5)C=C4)C=C3)C8=C2C=CC=C8)C)C=C1.[Br-].[Br-]
Formula	C₄₆H₃₈Cl₂N₄.2Br	M.Wt	877.5
Solubility	3mg/mL in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.1396 mL	5.698 mL	11.396 mL
	5 mM	0.2279 mL	1.1396 mL	2.2792 mL
	10 mM	0.114 mL	0.5698 mL	1.1396 mL

Molarity Calculator
Dilution Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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RSM-932A (Synonyms: TCD-717)

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