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LGB-321 HCl

    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 )


Price and Availability

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LGB-321 HCl is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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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


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


Technical Data

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).

Harmonized System Code:
2934.99.90.01


Additional Information

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


References

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.