LGB-321 dihydrochloride | CAS#1210417-75-6 | CAS# 1210416-93-5 | 1210417-75-6 | Pan-PIM inhibitor |

MedKoo Cat#: 406588 | Name: LGB-321 HCl

Description:

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

LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cell NHL. In vivo, LGB-321 is orally available, demonstrates efficacy in tumor xenografts and is well-tolerated within the therapeutic exposure range in mice. (source: Clin Cancer Res. 2014 Apr 1;20(7):1834-45 )

Chemical Structure

LGB-321 HCl

CAS#1210416-93-5 (2HCl)

Theoretical Analysis

MedKoo Cat#: 406588

Name: LGB-321 HCl

CAS#: 1210416-93-5 (2HCl)

Chemical Formula: C23H24Cl2F3N5O2

Exact Mass: 457.1726

Molecular Weight: 530.37

Elemental Analysis: C, 52.09; H, 4.56; Cl, 13.37; F, 10.75; N, 13.20; O, 6.03

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

1210416-93-5 (2HCl) 1469925-36-7 (HCl) 1210417-75-6 (free base)

Synonym

LGB321; LGB-321; LGB 321; LGB321 HCl

IUPAC/Chemical Name

N-(4-((3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide dihydrochloride

InChi Key

HFXMCBQUOIAWAM-OXKSASGCSA-N

InChi Code

InChI=1S/C23H22F3N5O2.2ClH/c1-12-10-31(11-16(27)22(12)32)19-7-8-28-9-18(19)30-23(33)17-6-5-15(26)21(29-17)20-13(24)3-2-4-14(20)25;;/h2-9,12,16,22,32H,10-11,27H2,1H3,(H,30,33);2*1H/t12-,16+,22+;;/m0../s1

SMILES Code

O=C(NC1=C(N2C[C@@H](N)[C@H](O)[C@@H](C)C2)C=CN=C1)C3=NC(C4=C(F)C=CC=C4F)=C(F)C=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, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO. or LGB321 may be also formulated for oral administration in 50mM Acetate buffer, pH4.

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

Related CAS# 1210416-93-5 ( LGB-321 dihydrochloride); 1469925-36-7 ( LGB-321 monhydrochloride) 1210417-75-6 (LGB-321 free base)

Product Data

Product Data

Instruction

View handling instruction

Biological target:

LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor).

In vitro activity:

GB321 is active on PIM2-dependent multiple myeloma cell lines, where it inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD. Broad cancer cell line profiling of LGB321 demonstrates limited activity in cell lines derived from solid tumors. Reference: Clin Cancer Res. 2014 Apr 1;20(7):1834-45. https://pubmed.ncbi.nlm.nih.gov/24474669/

In vivo activity:

Furthermore, this study demonstrates LGB321 activity in the KG-1 AML xenograft model, in which modulation of pharmacodynamics markers is predictive of efficacy. Finally, this study demonstrates that LGB321 synergizes with cytarabine in this model. Reference: Clin Cancer Res. 2014 Apr 1;20(7):1834-45. https://pubmed.ncbi.nlm.nih.gov/24474669/

Preparing Stock Solutions

The following data is based on the product molecular weight 530.37 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.

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. Garcia PD, Langowski JL, Wang Y, Chen M, Castillo J, Fanton C, Ison M, Zavorotinskaya T, Dai Y, Lu J, Niu XH, Basham S, Chan J, Yu J, Doyle M, Feucht P, Warne R, Narberes J, Tsang T, Fritsch C, Kauffmann A, Pfister E, Drueckes P, Trappe J, Wilson C, Han W, Lan J, Nishiguchi G, Lindvall M, Bellamacina C, Aycinena JA, Zang R, Holash J, Burger MT. Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers. Clin Cancer Res. 2014 Apr 1;20(7):1834-45. doi: 10.1158/1078-0432.CCR-13-2062. Epub 2014 Jan 28. PMID: 24474669.

In vitro protocol:

In vivo protocol:

1: Garcia PD, Langowski JL, Wang Y, Chen M, Castillo J, Fanton C, Ison M, Zavorotinskaya T, Dai Y, Lu J, Niu XH, Basham S, Chan J, Yu J, Doyle M, Feucht P, Warne R, Narberes J, Tsang T, Fritsch C, Kauffmann A, Pfister E, Drueckes P, Trappe J, Wilson C, Han W, Lan J, Nishiguchi G, Lindvall M, Bellamacina C, Aycinena JA, Zang R, Holash J, Burger MT. Pan-PIM kinase inhibition provides a novel therapy for treating hematologic cancers. Clin Cancer Res. 2014 Apr 1;20(7):1834-45. doi: 10.1158/1078-0432.CCR-13-2062. Epub 2014 Jan 28. PubMed PMID: 24474669.