MedKoo Cat#: 406562 | Name: LDN-212854
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Description:

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

LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2. LDN-212854 exhibits some selectivity for ALK2 in preference to other BMP type I receptors, ALK1 and ALK3, which may permit the interrogation of ALK2-mediated signaling, transcriptional activity, and function. LDN-212854 potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. The bone morphogenetic protein (BMP) signaling pathway has essential functions in development, homeostasis, and the normal and pathophysiologic remodeling of tissues. Small molecule inhibitors of the BMP receptor kinase family have been useful for probing physiologic functions of BMP signaling in vitro and in vivo and may have roles in the treatment of BMP-mediated diseases.

Chemical Structure

LDN-212854
LDN-212854
CAS#1432597-26-6

Theoretical Analysis

MedKoo Cat#: 406562

Name: LDN-212854

CAS#: 1432597-26-6

Chemical Formula: C25H22N6

Exact Mass: 406.1906

Molecular Weight: 406.48

Elemental Analysis: C, 73.87; H, 5.46; N, 20.67

Price and Availability

Size Price Availability Quantity
10mg USD 295.00 2 Weeks
25mg USD 600.00 2 Weeks
50mg USD 1,050.00 2 Weeks
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Related CAS #
No Data
Synonym
LDN212854; LDN 212854; LDN-212854.
IUPAC/Chemical Name
5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
InChi Key
BBDGBGOVJPEFBT-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2
SMILES Code
C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2
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, not in water
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
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Product Data
Biological target:
LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM).
In vitro activity:
LDN-212854 restored mature oligodendrocyte differentiation and blocked the formation of GFAP+ astrocytes from fibrinogen-treated OPCs in a dose-dependent manner (Fig. 3D). Reference: Brain. 2021 Sep 4;144(8):2291-2301. https://pubmed.ncbi.nlm.nih.gov/34426831/
In vivo activity:
In vivo, the BMP receptor inhibitor LDN-212854 successfully inhibited HCC tumor growth and angiogenesis by inhibiting BMP9-ID1 signaling in mice. Reference: Int J Mol Sci. 2022 Jan 27;23(3):1475. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8835914/
Solvent mg/mL mM
Solubility
DMF 10.0 24.60
DMSO 25.0 61.50
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 406.48 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. Petersen MA, Tognatta R, Meyer-Franke A, Bushong EA, Mendiola AS, Yan Z, Muthusamy A, Merlini M, Meza-Acevedo R, Cabriga B, Zhou Y, Thomas R, Ryu JK, Lassmann H, Ellisman MH, Akassoglou K. BMP receptor blockade overcomes extrinsic inhibition of remyelination and restores neurovascular homeostasis. Brain. 2021 Sep 4;144(8):2291-2301. doi: 10.1093/brain/awab106. PMID: 34426831; PMCID: PMC8418337. 2. Chen H, Nio K, Yamashita T, Okada H, Li R, Suda T, Li Y, Doan PTB, Seki A, Nakagawa H, Toyama T, Terashima T, Iida N, Shimakami T, Takatori H, Kawaguchi K, Sakai Y, Yamashita T, Mizukoshi E, Honda M, Kaneko S. BMP9-ID1 signaling promotes EpCAM-positive cancer stem cell properties in hepatocellular carcinoma. Mol Oncol. 2021 Aug;15(8):2203-2218. doi: 10.1002/1878-0261.12963. Epub 2021 May 2. PMID: 33834612; PMCID: PMC8333780. 3. Chen H, Nio K, Tang H, Yamashita T, Okada H, Li Y, Doan PTB, Li R, Lv J, Sakai Y, Yamashita T, Mizukoshi E, Honda M, Kaneko S. BMP9-ID1 Signaling Activates HIF-1α and VEGFA Expression to Promote Tumor Angiogenesis in Hepatocellular Carcinoma. Int J Mol Sci. 2022 Jan 27;23(3):1475. doi: 10.3390/ijms23031475. PMID: 35163396; PMCID: PMC8835914. 4. Mohedas AH, Xing X, Armstrong KA, Bullock AN, Cuny GD, Yu PB. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem Biol. 2013;8(6):1291-302. doi: 10.1021/cb300655w. Epub 2013 Apr 30. PMID: 23547776; PMCID: PMC3901569.
In vitro protocol:
1. Petersen MA, Tognatta R, Meyer-Franke A, Bushong EA, Mendiola AS, Yan Z, Muthusamy A, Merlini M, Meza-Acevedo R, Cabriga B, Zhou Y, Thomas R, Ryu JK, Lassmann H, Ellisman MH, Akassoglou K. BMP receptor blockade overcomes extrinsic inhibition of remyelination and restores neurovascular homeostasis. Brain. 2021 Sep 4;144(8):2291-2301. doi: 10.1093/brain/awab106. PMID: 34426831; PMCID: PMC8418337. 2. Chen H, Nio K, Yamashita T, Okada H, Li R, Suda T, Li Y, Doan PTB, Seki A, Nakagawa H, Toyama T, Terashima T, Iida N, Shimakami T, Takatori H, Kawaguchi K, Sakai Y, Yamashita T, Mizukoshi E, Honda M, Kaneko S. BMP9-ID1 signaling promotes EpCAM-positive cancer stem cell properties in hepatocellular carcinoma. Mol Oncol. 2021 Aug;15(8):2203-2218. doi: 10.1002/1878-0261.12963. Epub 2021 May 2. PMID: 33834612; PMCID: PMC8333780.
In vivo protocol:
1. Chen H, Nio K, Tang H, Yamashita T, Okada H, Li Y, Doan PTB, Li R, Lv J, Sakai Y, Yamashita T, Mizukoshi E, Honda M, Kaneko S. BMP9-ID1 Signaling Activates HIF-1α and VEGFA Expression to Promote Tumor Angiogenesis in Hepatocellular Carcinoma. Int J Mol Sci. 2022 Jan 27;23(3):1475. doi: 10.3390/ijms23031475. PMID: 35163396; PMCID: PMC8835914. 2. Mohedas AH, Xing X, Armstrong KA, Bullock AN, Cuny GD, Yu PB. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem Biol. 2013;8(6):1291-302. doi: 10.1021/cb300655w. Epub 2013 Apr 30. PMID: 23547776; PMCID: PMC3901569.
1: Mohedas AH, Xing X, Armstrong KA, Bullock AN, Cuny GD, Yu PB. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem Biol. 2013;8(6):1291-302. doi: 10.1021/cb300655w. Epub 2013 Apr 30. PubMed PMID: 23547776; PubMed Central PMCID: PMC3901569.