RBC8
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MedKoo CAT#: 406737

CAS#: 361185-42-4

Description: RBC8 is a RalA and RalB GTPase inhibitor (EC50 ~3.5 μM). RBC8 suppresses growth of xenograft tumors in mice. e Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis. Chemicals that block Ral function would be valuable as research tools and for cancer therapeutics.


Chemical Structure

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RBC8
CAS# 361185-42-4

Theoretical Analysis

MedKoo Cat#: 406737
Name: RBC8
CAS#: 361185-42-4
Chemical Formula: C25H20N4O3
Exact Mass: 424.15
Molecular Weight: 424.460
Elemental Analysis: C, 70.74; H, 4.75; N, 13.20; O, 11.31

Price and Availability

Size Price Availability Quantity
100mg USD 950
200mg USD 1650
500mg USD 2250
1g USD 3350
2g USD 5150
5g USD 8450
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Synonym: RBC8; RBC-8; RBC 8.

IUPAC/Chemical Name: 6-Amino-4-(2,5-dimethoxyphenyl)-1,4-dihydro-3-(2-naphthalenyl)pyrano[2,3-c]pyrazole-5-carbonitrile

InChi Key: CLMQBVUFKIKYLU-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H20N4O3/c1-30-17-9-10-20(31-2)18(12-17)21-19(13-26)24(27)32-25-22(21)23(28-29-25)16-8-7-14-5-3-4-6-15(14)11-16/h3-12,21H,27H2,1-2H3,(H,28,29)

SMILES Code: N#CC(C1C2=CC(OC)=CC=C2OC)=C(N)OC3=C1C(C4=CC=C5C=CC=CC5=C4)=NN3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, DMF, and ethanol

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO, DMF, and ethanol

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: RBC8 prevents binding of the GTPase to the Ral-binding protein. RBC8 prevented Ral-mediated spreading of murine embryonic fibroblasts, blocked anchorage-independent growth of H2122 and H358 lung cancer cell lines (IC50s = 3.5 and 3.4 µM, respectively), and inhibited the growth of H2122 lung cancer xenografts in mice (50 mg/kg i.p.).
In vitro activity: To be determined
In vivo activity: RBC8 and BQU57 show selectivity for Ral relative to the GTPases Ras and RhoA and inhibit tumour xenograft growth to a similar extent to the depletion of Ral using RNA interference. Reference: Nature. 2014 Nov 20;515(7527):443-7. https://pubmed.ncbi.nlm.nih.gov/25219851/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 30.0 70.68
DMSO 30.0 70.68
Ethanol 0.3 0.59

Preparing Stock Solutions

The following data is based on the product molecular weight 424.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Walsh TG, Wersäll A, Poole AW. Characterisation of the Ral GTPase inhibitor RBC8 in human and mouse platelets. Cell Signal. 2019 Jul;59:34-40. doi: 10.1016/j.cellsig.2019.03.015. Epub 2019 Mar 14. PMID: 30880223; PMCID: PMC6510928. 2. Yan C, Liu D, Li L, Wempe MF, Guin S, Khanna M, Meier J, Hoffman B, Owens C, Wysoczynski CL, Nitz MD, Knabe WE, Ahmed M, Brautigan DL, Paschal BM, Schwartz MA, Jones DN, Ross D, Meroueh SO, Theodorescu D. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7. doi: 10.1038/nature13713. Epub 2014 Sep 14. PMID: 25219851; PMCID: PMC4351747.
In vitro protocol: To be determined
In vivo protocol: 1. Walsh TG, Wersäll A, Poole AW. Characterisation of the Ral GTPase inhibitor RBC8 in human and mouse platelets. Cell Signal. 2019 Jul;59:34-40. doi: 10.1016/j.cellsig.2019.03.015. Epub 2019 Mar 14. PMID: 30880223; PMCID: PMC6510928. 2. Yan C, Liu D, Li L, Wempe MF, Guin S, Khanna M, Meier J, Hoffman B, Owens C, Wysoczynski CL, Nitz MD, Knabe WE, Ahmed M, Brautigan DL, Paschal BM, Schwartz MA, Jones DN, Ross D, Meroueh SO, Theodorescu D. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7. doi: 10.1038/nature13713. Epub 2014 Sep 14. PMID: 25219851; PMCID: PMC4351747.

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1: Walsh TG, Wersäll A, Poole AW. Characterisation of the Ral GTPase inhibitor RBC8 in human and mouse platelets. Cell Signal. 2019 Jul;59:34-40. doi: 10.1016/j.cellsig.2019.03.015. Epub 2019 Mar 14. PMID: 30880223; PMCID: PMC6510928.

2: Kodama T, Bard-Chapeau EA, Newberg JY, Kodama M, Rangel R, Yoshihara K, Ward JM, Jenkins NA, Copeland NG. Two-step Forward Genetic Screen in Mice Identifies Ral GTPase-activating Proteins as Suppressors of Hepatocellular Carcinoma. Gastroenterology. 2016 May 10. pii: S0016-5085(16)34392-X. doi: 10.1053/j.gastro.2016.04.040. [Epub ahead of print] PubMed PMID: 27178121.

3: Gu C, Feng M, Yin Z, Luo X, Yang J, Li Y, Li T, Wang R, Fei J. RalA, a GTPase targeted by miR‑181a, promotes transformation and progression by activating the Ras‑related signaling pathway in chronic myelogenous leukemia. Oncotarget. 2016 Mar 8. doi: 10.18632/oncotarget.7987. [Epub ahead of print] PubMed PMID: 26967392.


4: Yan C, Liu D, Li L, Wempe MF, Guin S, Khanna M, Meier J, Hoffman B, Owens C, Wysoczynski CL, Nitz MD, Knabe WE, Ahmed M, Brautigan DL, Paschal BM, Schwartz MA, Jones DN, Ross D, Meroueh SO, Theodorescu D. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7. doi: 10.1038/nature13713. Epub 2014 Sep 14. PubMed PMID: 25219851; PubMed Central PMCID: PMC4351747.