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MedKoo Cat#: 527769 | Name: SB505124 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SB05124 HCl is an inhibitor of activin receptor-like kinase (ALK) 5.

Chemical Structure

SB505124 HCl
SB505124 HCl
CAS#356559-13-2 (HCl)

Theoretical Analysis

MedKoo Cat#: 527769

Name: SB505124 HCl

CAS#: 356559-13-2 (HCl)

Chemical Formula: C20H22ClN3O2

Exact Mass: 0.0000

Molecular Weight: 371.87

Elemental Analysis: C, 64.60; H, 5.96; Cl, 9.53; N, 11.30; O, 8.60

Price and Availability

Size Price Availability Quantity
5mg USD 315.00 2 weeks
10mg USD 550.00 2 Weeks
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Related CAS #
356559-13-2 (HCl) 694433-59-5 (free base)
Synonym
SB505124 HCl; SB 505124 HCl; SB-505124 HCl
IUPAC/Chemical Name
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride
InChi Key
BTUOOXPZOVNPMF-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H21N3O2.ClH/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15;/h5-10H,11H2,1-4H3,(H,22,23);1H
SMILES Code
CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1.[H]Cl
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
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Product Data
Instruction
View handling instruction
Biological target:
SB505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
In vitro activity:
Pharmacological inhibition of the ACVR1C receptor using SB505124 significantly reduced growth and invasion of cultured retinoblastoma cells in a dose-dependent manner. In WERI Rb1 cells, growth was potently suppressed, and in Y79 cells, growth was almost completely suppressed at concentrations. HSJD-RBVS-10 cells were less responsive to SB505124-mediated growth inhibition, but growth was still inhibited. Reference: Oncogene. 2019 Mar; 38(12): 2056–2075. https://pubmed.ncbi.nlm.nih.gov/30401983/
In vivo activity:
In this study, SB505124 effectively alleviated symptoms of cancer-related anemia (CRA). SB505124 notably improved erythrocyte levels, restored hindered hematopoiesis, and enhanced the bone marrow's hematopoietic stem cell (HSC) niche. SB505124 has potential as a safe and effective treatment for CRA and potentially other cancer-related disorders. Reference: Stem Cell Res Ther. 2021; 12: 65. https://pubmed.ncbi.nlm.nih.gov/33461597/
Solvent mg/mL mM
Solubility
DMSO 50.0 134.15
Methanol 125.0 336.16
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 371.87 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. Asnaghi L, White DT, Key N, Choi J, Mahale A, Alkatan H, Edward DP, Elkhamary SM, Al-Mesfer S, Maktabi A, Hurtado CG, Lee GY, Carcaboso AM, Mumm JS, Safieh LA, Eberhart CG. ACVR1C/SMAD2 signaling promotes invasion and growth in retinoblastoma. Oncogene. 2019 Mar;38(12):2056-2075. doi: 10.1038/s41388-018-0543-2. Epub 2018 Nov 6. PMID: 30401983; PMCID: PMC6430693. 2. Liu Y, Sharma T, Chen IP, Reichenberger E, Ueki Y, Arif Y, Parisi D, Maye P. Rescue of a cherubism bone marrow stromal culture phenotype by reducing TGFβ signaling. Bone. 2018 Jun;111:28-35. doi: 10.1016/j.bone.2018.03.009. Epub 2018 Mar 9. PMID: 29530719; PMCID: PMC5924722. 3. Wang B, Wang Y, Chen H, Yao S, Lai X, Qiu Y, Cai J, Huang Y, Wei X, Guan Y, Wang T, Wang J, Xiang AP. Inhibition of TGFβ improves hematopoietic stem cell niche and ameliorates cancer-related anemia. Stem Cell Res Ther. 2021 Jan 18;12(1):65. doi: 10.1186/s13287-020-02120-9. PMID: 33461597; PMCID: PMC7814632. 4. Zhang H, Chen S, Shang C, Wu X, Wang Y, Li G. Interplay between Lefty and Nodal signaling is essential for the organizer and axial formation in amphioxus embryos. Dev Biol. 2019 Dec 1;456(1):63-73. doi: 10.1016/j.ydbio.2019.08.006. Epub 2019 Aug 13. PMID: 31419410.
In vitro protocol:
1. Asnaghi L, White DT, Key N, Choi J, Mahale A, Alkatan H, Edward DP, Elkhamary SM, Al-Mesfer S, Maktabi A, Hurtado CG, Lee GY, Carcaboso AM, Mumm JS, Safieh LA, Eberhart CG. ACVR1C/SMAD2 signaling promotes invasion and growth in retinoblastoma. Oncogene. 2019 Mar;38(12):2056-2075. doi: 10.1038/s41388-018-0543-2. Epub 2018 Nov 6. PMID: 30401983; PMCID: PMC6430693. 2. Liu Y, Sharma T, Chen IP, Reichenberger E, Ueki Y, Arif Y, Parisi D, Maye P. Rescue of a cherubism bone marrow stromal culture phenotype by reducing TGFβ signaling. Bone. 2018 Jun;111:28-35. doi: 10.1016/j.bone.2018.03.009. Epub 2018 Mar 9. PMID: 29530719; PMCID: PMC5924722.
In vivo protocol:
1. Wang B, Wang Y, Chen H, Yao S, Lai X, Qiu Y, Cai J, Huang Y, Wei X, Guan Y, Wang T, Wang J, Xiang AP. Inhibition of TGFβ improves hematopoietic stem cell niche and ameliorates cancer-related anemia. Stem Cell Res Ther. 2021 Jan 18;12(1):65. doi: 10.1186/s13287-020-02120-9. PMID: 33461597; PMCID: PMC7814632. 2. Zhang H, Chen S, Shang C, Wu X, Wang Y, Li G. Interplay between Lefty and Nodal signaling is essential for the organizer and axial formation in amphioxus embryos. Dev Biol. 2019 Dec 1;456(1):63-73. doi: 10.1016/j.ydbio.2019.08.006. Epub 2019 Aug 13. PMID: 31419410.
1: Go YY, Kim SE, Cho GJ, Chae SW, Song JJ. Differential effects of amnion and chorion membrane extracts on osteoblast-like cells due to the different growth factor composition of the extracts. PLoS One. 2017 Aug 10;12(8):e0182716. doi: 10.1371/journal.pone.0182716. eCollection 2017. PubMed PMID: 28797129; PubMed Central PMCID: PMC5552222. 2: Zhang H, Du L, Zhong Y, Flanders KC, Roberts JD Jr. Transforming growth factor-β stimulates Smad1/5 signaling in pulmonary artery smooth muscle cells and fibroblasts of the newborn mouse through ALK1. Am J Physiol Lung Cell Mol Physiol. 2017 Sep 1;313(3):L615-L627. doi: 10.1152/ajplung.00079.2017. Epub 2017 Jun 22. PubMed PMID: 28642261; PubMed Central PMCID: PMC5625261. 3: Kim BH, Guardia Clausi M, Frondelli M, Nnah IC, Saqcena C, Dobrowolski R, Levison SW. Age-Dependent Effects of ALK5 Inhibition and Mechanism of Neuroprotection in Neonatal Hypoxic-Ischemic Brain Injury. Dev Neurosci. 2017;39(1-4):338-351. doi: 10.1159/000477490. Epub 2017 Jun 20. PubMed PMID: 28628913; PubMed Central PMCID: PMC5555313. 4: van Caam A, Madej W, Garcia de Vinuesa A, Goumans MJ, Ten Dijke P, Blaney Davidson E, van der Kraan P. TGFβ1-induced SMAD2/3 and SMAD1/5 phosphorylation are both ALK5-kinase-dependent in primary chondrocytes and mediated by TAK1 kinase activity. Arthritis Res Ther. 2017 May 31;19(1):112. doi: 10.1186/s13075-017-1302-4. PubMed PMID: 28569204; PubMed Central PMCID: PMC5452635. 5: Jiang J, Zhang Y, Peng K, Wang Q, Hong X, Li H, Fan G, Zhang Z, Gong T, Sun X. Combined delivery of a TGF-β inhibitor and an adenoviral vector expressing interleukin-12 potentiates cancer immunotherapy. Acta Biomater. 2017 Oct 1;61:114-123. doi: 10.1016/j.actbio.2017.05.009. Epub 2017 May 5. PubMed PMID: 28483693. 6: Wang J, Chen Y, Gu D, Zhang G, Chen J, Zhao J, Wu P. Ketamine-induced bladder fibrosis involves epithelial-to-mesenchymal transition mediated by transforming growth factor-β1. Am J Physiol Renal Physiol. 2017 Oct 1;313(4):F961-F972. doi: 10.1152/ajprenal.00686.2016. Epub 2017 Mar 22. PubMed PMID: 28331066. 7: Chang HM, Fang Y, Liu PP, Cheng JC, Yang X, Leung PC. Connective tissue growth factor mediates growth differentiation factor 8-induced increase of lysyl oxidase activity in human granulosa-lutein cells. Mol Cell Endocrinol. 2016 Oct 15;434:186-98. doi: 10.1016/j.mce.2016.07.007. Epub 2016 Jul 5. PubMed PMID: 27392496. 8: Terakawa J, Rocchi A, Serna VA, Bottinger EP, Graff JM, Kurita T. FGFR2IIIb-MAPK Activity Is Required for Epithelial Cell Fate Decision in the Lower Müllerian Duct. Mol Endocrinol. 2016 Jul;30(7):783-95. doi: 10.1210/me.2016-1027. Epub 2016 May 10. PubMed PMID: 27164167; PubMed Central PMCID: PMC4926232. 9: Rateitschak K, Kaderali L, Wolkenhauer O, Jaster R. Autocrine TGF-β/ZEB/microRNA-200 signal transduction drives epithelial-mesenchymal transition: Kinetic models predict minimal drug dose to inhibit metastasis. Cell Signal. 2016 Aug;28(8):861-70. doi: 10.1016/j.cellsig.2016.03.002. Epub 2016 Mar 19. PubMed PMID: 27000495. 10: Guardia Clausi M, Levison SW. Delayed ALK5 inhibition improves functional recovery in neonatal brain injury. J Cereb Blood Flow Metab. 2017 Mar;37(3):787-800. doi: 10.1177/0271678X16638669. Epub 2016 Jul 20. PubMed PMID: 26984936; PubMed Central PMCID: PMC5363459. 11: Kim H, Kei K, Sonn JK. Staurosporine induces chondrogenesis of chick embryo wing bud mesenchyme in monolayer cultures through canonical and non-canonical TGF-β pathways. In Vitro Cell Dev Biol Anim. 2016 Jan;52(1):120-9. doi: 10.1007/s11626-015-9954-3. Epub 2015 Oct 1. PubMed PMID: 26427712. 12: Jiang J, Zhang Y, Zhang Q, Li Y, Gong T, Zhang Z, Ding R, Sun X. Development and validation of an LC-MS/MS method for the determination of SB-505124 in rat plasma: Application to pharmacokinetic study. J Pharm Biomed Anal. 2016 Jan 5;117:205-9. doi: 10.1016/j.jpba.2015.09.002. Epub 2015 Sep 3. PubMed PMID: 26363490. 13: Li S, Niu G, Wu Y, Du G, Huang C, Yin X, Liu Z, Song C, Leng H. Vitamin D prevents articular cartilage erosion by regulating collagen II turnover through TGF-β1 in ovariectomized rats. Osteoarthritis Cartilage. 2016 Feb;24(2):345-53. doi: 10.1016/j.joca.2015.08.013. Epub 2015 Sep 4. PubMed PMID: 26343586. 14: Tekari A, Luginbuehl R, Hofstetter W, Egli RJ. Transforming growth factor beta signaling is essential for the autonomous formation of cartilage-like tissue by expanded chondrocytes. PLoS One. 2015 Mar 16;10(3):e0120857. doi: 10.1371/journal.pone.0120857. eCollection 2015. PubMed PMID: 25775021; PubMed Central PMCID: PMC4361600. 15: Brown KM, Suvorova E, Farrell A, McLain A, Dittmar A, Wiley GB, Marth G, Gaffney PM, Gubbels MJ, White M, Blader IJ. Forward genetic screening identifies a small molecule that blocks Toxoplasma gondii growth by inhibiting both host- and parasite-encoded kinases. PLoS Pathog. 2014 Jun 12;10(6):e1004180. doi: 10.1371/journal.ppat.1004180. eCollection 2014 Jun. PubMed PMID: 24945800; PubMed Central PMCID: PMC4055737. 16: Zhang S, Sun WY, Wu JJ, Wei W. TGF-β signaling pathway as a pharmacological target in liver diseases. Pharmacol Res. 2014 Jul;85:15-22. doi: 10.1016/j.phrs.2014.05.005. Epub 2014 May 17. Review. PubMed PMID: 24844437. 17: Uchinaka A, Kawaguchi N, Mori S, Hamada Y, Miyagawa S, Saito A, Sawa Y, Matsuura N. Tissue inhibitor of metalloproteinase-1 and -3 improves cardiac function in an ischemic cardiomyopathy model rat. Tissue Eng Part A. 2014 Nov;20(21-22):3073-84. doi: 10.1089/ten.TEA.2013.0763. Epub 2014 Jun 16. PubMed PMID: 24814095; PubMed Central PMCID: PMC4229714. 18: Choi SG, Wang Q, Jia J, Pincas H, Turgeon JL, Sealfon SC. Growth differentiation factor 9 (GDF9) forms an incoherent feed-forward loop modulating follicle-stimulating hormone β-subunit (FSHβ) gene expression. J Biol Chem. 2014 Jun 6;289(23):16164-75. doi: 10.1074/jbc.M113.537696. Epub 2014 Apr 28. PubMed PMID: 24778184; PubMed Central PMCID: PMC4047387. 19: Wu TH, Chou YW, Chiu PH, Tang MJ, Hu CW, Yeh ML. Validation of the effects of TGF-β1 on tumor recurrence and prognosis through tumor retrieval and cell mechanical properties. Cancer Cell Int. 2014 Mar 3;14(1):20. doi: 10.1186/1475-2867-14-20. PubMed PMID: 24581230; PubMed Central PMCID: PMC3973896. 20: Mikhailova A, Ilmarinen T, Uusitalo H, Skottman H. Small-molecule induction promotes corneal epithelial cell differentiation from human induced pluripotent stem cells. Stem Cell Reports. 2014 Feb 6;2(2):219-31. doi: 10.1016/j.stemcr.2013.12.014. eCollection 2014 Feb 11. PubMed PMID: 24527395; PubMed Central PMCID: PMC3923224.

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DWN-723-23

DWN-723-23