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MedKoo Cat#: 581052 | Name: LGH447 dihydrochloride
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Description:

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

LGH447 dihydrochloride is potent and specific pan-PIM inhibitor that inhibits proliferation of several AML cell lines showing dual antitumoral and bone antiresorptive effects. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency.

Chemical Structure

LGH447 dihydrochloride
LGH447 dihydrochloride
CAS#1820565-69-2 (2HCl)

Theoretical Analysis

MedKoo Cat#: 581052

Name: LGH447 dihydrochloride

CAS#: 1820565-69-2 (2HCl)

Chemical Formula: C24H25Cl2F3N4O

Exact Mass: 0.0000

Molecular Weight: 513.39

Elemental Analysis: C, 56.15; H, 4.91; Cl, 13.81; F, 11.10; N, 10.91; O, 3.12

Price and Availability

Size Price Availability Quantity
5mg USD 570.00 2 Weeks
10mg USD 1,050.00 2 Weeks
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Related CAS #
1210416-52-6 (HCl) 1820565-69-2 (2HCl) 1210608-43-7 (free base)
Synonym
LGH447 Hydrochloride, LGH447; LGH-447; LGH 447; PIM-447 HCl; PIM-447; PIM 447; PIM447.
IUPAC/Chemical Name
N-[4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]pyridin-3-yl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide dihydrochloride
InChi Key
BVRSHQQSBGCMJE-ALGQTRDQSA-N
InChi Code
InChI=1S/C24H23F3N4O.2ClH/c1-13-9-14(11-15(28)10-13)16-7-8-29-12-21(16)31-24(32)20-6-5-19(27)23(30-20)22-17(25)3-2-4-18(22)26;;/h2-8,12-15H,9-11,28H2,1H3,(H,31,32);2*1H/t13-,14+,15-;;/m0../s1
SMILES Code
O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=C([C@H]4C[C@@H](N)C[C@@H](C)C4)C=CN=C3.[H]Cl.[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:
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively.
In vitro activity:
PIM447 significantly decreased the viability, proliferation, and motility of HuH6 and COA67 cells. Apoptosis significantly increased following PIM447 treatment. PIM447 had a significant impact on tumor cell stemness as evidenced by decreased expression of CD133 and reduced ability of HuH6 and COA67 cells to form tumorspheres. Reference: J Pediatr Surg. 2021 Jun;56(6):1157-1164. https://pubmed.ncbi.nlm.nih.gov/33762119/
In vivo activity:
Finally, PIM447 significantly reduced the tumor burden and prevented tumor-associated bone loss in a disseminated murine model of human myeloma. Reference: Clin Cancer Res. 2017 Jan 1;23(1):225-238. https://pubmed.ncbi.nlm.nih.gov/27440267/
Solvent mg/mL mM comments
Solubility
Water 50.0 97.39
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 513.39 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. Wadhwani N, Markert HR, Marayati R, Bownes LV, Quinn CH, Aye JM, Stewart JE, Yoon KJ, Beierle EA. PIM447 inhibits oncogenesis and potentiates cisplatin effects in hepatoblastoma. J Pediatr Surg. 2021 Jun;56(6):1157-1164. doi: 10.1016/j.jpedsurg.2021.02.039. Epub 2021 Feb 24. PMID: 33762119; PMCID: PMC8131223. 2. Leung MS, Chan KK, Dai WJ, Wong CY, Au KY, Wong PY, Wong CC, Lee TK, Ng IO, Kao WJ, Lo RC. Anti-tumour effects of PIM kinase inhibition on progression and chemoresistance of hepatocellular carcinoma. J Pathol. 2020 Sep;252(1):65-76. doi: 10.1002/path.5492. Epub 2020 Jul 31. PMID: 32558942. 3. Paíno T, Garcia-Gomez A, González-Méndez L, San-Segundo L, Hernández-García S, López-Iglesias AA, Algarín EM, Martín-Sánchez M, Corbacho D, Ortiz-de-Solorzano C, Corchete LA, Gutiérrez NC, Maetos MV, Garayoa M, Ocio EM. The Novel Pan-PIM Kinase Inhibitor, PIM447, Displays Dual Antimyeloma and Bone-Protective Effects, and Potently Synergizes with Current Standards of Care. Clin Cancer Res. 2017 Jan 1;23(1):225-238. doi: 10.1158/1078-0432.CCR-16-0230. Epub 2016 Jul 20. PMID: 27440267.
In vitro protocol:
1. Wadhwani N, Markert HR, Marayati R, Bownes LV, Quinn CH, Aye JM, Stewart JE, Yoon KJ, Beierle EA. PIM447 inhibits oncogenesis and potentiates cisplatin effects in hepatoblastoma. J Pediatr Surg. 2021 Jun;56(6):1157-1164. doi: 10.1016/j.jpedsurg.2021.02.039. Epub 2021 Feb 24. PMID: 33762119; PMCID: PMC8131223. 2. Leung MS, Chan KK, Dai WJ, Wong CY, Au KY, Wong PY, Wong CC, Lee TK, Ng IO, Kao WJ, Lo RC. Anti-tumour effects of PIM kinase inhibition on progression and chemoresistance of hepatocellular carcinoma. J Pathol. 2020 Sep;252(1):65-76. doi: 10.1002/path.5492. Epub 2020 Jul 31. PMID: 32558942.
In vivo protocol:
1. Paíno T, Garcia-Gomez A, González-Méndez L, San-Segundo L, Hernández-García S, López-Iglesias AA, Algarín EM, Martín-Sánchez M, Corbacho D, Ortiz-de-Solorzano C, Corchete LA, Gutiérrez NC, Maetos MV, Garayoa M, Ocio EM. The Novel Pan-PIM Kinase Inhibitor, PIM447, Displays Dual Antimyeloma and Bone-Protective Effects, and Potently Synergizes with Current Standards of Care. Clin Cancer Res. 2017 Jan 1;23(1):225-238. doi: 10.1158/1078-0432.CCR-16-0230. Epub 2016 Jul 20. PMID: 27440267.
1: Burger MT, Nishiguchi G, Han W, Lan J, Simmons R, Atallah G, Ding Y, Tamez V, Zhang Y, Mathur M, Muller K, Bellamacina C, Lindvall MK, Zang R, Huh K, Feucht P, Zavorotinskaya T, Dai Y, Basham S, Chan J, Ginn E, Aycinena A, Holash J, Castillo J, Langowski JL, Wang Y, Chen MY, Lambert A, Fritsch C, Kauffmann A, Pfister E, Vanasse KG, Garcia PD. Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)- 5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. J Med Chem. 2015 Nov 12;58(21):8373-86. doi: 10.1021/acs.jmedchem.5b01275. Epub 2015 Oct 27. PubMed PMID: 26505898. 2: Paíno T, Garcia-Gomez A, González-Méndez L, San-Segundo L, Hernández-García S, López-Iglesias AA, Algarín EM, Martín-Sánchez M, Corbacho D, Ortiz-de-Solorzano C, Corchete LA, Gutiérrez NC, Maetos MV, Garayoa M, Ocio EM. The Novel Pan-PIM Kinase Inhibitor, PIM447, Displays Dual Antimyeloma and Bone-Protective Effects, and Potently Synergizes with Current Standards of Care. Clin Cancer Res. 2017 Jan 1;23(1):225-238. doi: 10.1158/1078-0432.CCR-16-0230. Epub 2016 Jul 20. PubMed PMID: 27440267.