PIM447 free base · Synonyms: LGH447

PIM447 is a potent, orally available, and selective pan-PIM kinase inhibitor.

For research use only. Not for human or veterinary use.

Target Pim Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

PIM447 structure

CAS No.: 1210608-43-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 450.00	BP-01854-25mg	In stock	Get quote
50 mg	USD 598.00	BP-01854-50mg	In stock	Get quote
100 mg	USD 960.00	BP-01854-100mg	In stock	Get quote
250 mg	USD 1,520.00	BP-01854-250mg	In stock	Get quote
500 mg	USD 2,280.00	BP-01854-500mg	In stock	Get quote
1 g	Inquire	BP-01854-1g	In stock	Inquire

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Description

PIM447 (LGH447) 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. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.

Biological activity

In Vitro PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells. PIM447 (10 μM; 6-24 hours) induces apoptosis. PIM447 (0.1-10 μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (S and G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses. In Vivo PIM447 (100 mg/kg; p.o.; 5 times for a week) reduces tumor burden.

Identifiers

SMILES: C[C@@H]1C[C@H](N)C[C@@H](C1)C1=C(NC(=O)C2=CC=C(F)C(=N2)C2=C(F)C=CC=C2F)C=NC=C1
InChIKey: VRQXRVAKPDCRCI-ZNMIVQPWSA-N

Specifications

MW (average): 440.4608
Formula: C₂₄H₂₃F₃N₄O
CAS No.: 1210608-43-7
Physical state: Solid
Color: white to off-white
Shipping: 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: Powder 4℃, sealed storage, away from moisture; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Burger MT, et al. 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 Inhibito

[2]. Paíno T et al. The novel pan-PIM kinase inhibitor, PIM447, displays dual anti-myeloma and bone protective effects, and potently synergizes with current standards of care. Clin Cancer Res. 2016 Jul 20.

[3]. Peters TL et al. Control of translational activation by PIM kinase in activated B-cell diffuse large B-cell lymphoma confers sensitivity to inhibition by PIM447. Oncotarget. 2016 Aug 20

Same target

Search Pim

Same research area

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