Comparison

(1S,3R,5R)-PIM447 dihydrochloride

Item no. V2738-25mg
Manufacturer InvivoChem LLC
CASRN NULL
Amount 25 mg
Quantity options 100 mg 10 mg 250 mg 50 mg 5 mg
Category
Type Biochemicals
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Available
Description
InvivoChem Cat #:V2738CAS #:N/APurity >=98%

Description: (1S, 3R, 5R)-PIM447 dihydrochloride a potent PIM inhibitor extracted with IC50 values of 0.095 uM for Pim1, 0.522 uM for Pim2 and 0.369 uM for Pim3. It is the isomer of PIM447 (also known as LGH447) which is a novel and potent pan-PIM (proviral insertion site of Moloney murine leukemia) kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3beta, PKN1, and PKCtau, but at a significantly lower potency with IC50 between 1 and 5 uM (> 105-fold differential relative to the Ki on PIMs). PIM447 is cytotoxic for myeloma cells due to cell cycle disruption and induction of apoptosis mediated by a decrease in phospho-Bad (Ser112) and c-Myc levels and the inhibition of mTORC1 pathway. PIM447 is currently undergoing several clinical trials.

References: J Med Chem. 2015 Nov 12; 58(21):8373-86; Clin Cancer Res. 2017 Jan 1; 23(1):225-238.

Related CAS #: 1820565-69-2 (2HCl); 1210608-43-7 (free base); 1210416-52-6 (HCl)

: 1820565-69-2 (2HCl); 1210608-43-7 (free base); 1210416-52-6 (HCl)
Molecular Weight (MW)
513.39
Formula
C24H25Cl2F3N4O
CAS No.
1210608-43-7 (free base); 1210416-52-6 (HCl); 1820565-69-2 (2HCl)
Storage
-20C for 3 years in powder form
-80C for 2 years in solvent
Solubility (In vitro)
DMSO: 88 mg/mL (184.5 mM)
Water: < 1 mg/mL
Ethanol: 88 mg/mL (184.5 mM)
SMILES Code
O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=C([CH]4C[CH](N)C[CH](C)C4)C=CN=C3.[H]Cl.[H]Cl
Synonyms
(1S, 3R, 5R)-PIM447 dihydrochloride; (1S, 3R, 5R)-PIM-447; (1S, 3R, 5R)-PIM 447; (1S, 3R, 5R)-LGH-447 dihydrochloride; (1S, 3R, 5R)-LGH 447; (1S, 3R, 5R)-LGH447

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 25 mg
Available: In stock
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