WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406588
CAS#: 1210416-93-5 (2HCl)
Description: 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 )
MedKoo Cat#: 406588
Name: LGB-321 HCl
CAS#: 1210416-93-5 (2HCl)
Chemical Formula: C23H24Cl2F3N5O2
Exact Mass: 457.1726
Molecular Weight: 530.3732
Elemental Analysis: C, 52.09; H, 4.56; Cl, 13.37; F, 10.75; N, 13.20; O, 6.03
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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
| 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/ |
The following data is based on the product molecular weight 530.3732 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: | 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 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. PMID: 24474669. |
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.
Related CAS#
1210416-93-5 ( LGB-321 dihydrochloride);
1469925-36-7 ( LGB-321 monhydrochloride)
1210417-75-6 (LGB-321 free base)
