|Description||ABTL-0812 is an orally bioavailable, lipid analogue and inhibitor of raptor-mammalian target of rapamycin (mTOR), rictor-mTOR and dihydrofolate reductase with potential antineoplastic activity. It binds to and inhibits both mTORC1 and mTORC2, which may result in apoptosis and a decrease in proliferation in mTORC1/2-expressing tumor cells upon oral administration. It was developed by Ability Pharmaceuticals and is in phase I/II clinical trials for the treatment of solid tumors. It received orphan drug designation in the E.U. and in the U.S. for the treatment of neuroblastoma in 2015.|
|Solubility||Soluble in DMSO, not in water|
|Application||ABTL-0812 has potential antineoplastic activity. It is used for the treatment of solid tumors|
|Quality Standard||In-house standard|
|Boiling Point||409.7±30.0 °C | Condition: Press: 760 Torr|
|Density||0.970±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
|Current Developer||ABTL-0812 was developed by Ability Pharmaceuticals and is in phase I/II clinical trials. It received orphan drug designation in the E.U. and in the U.S. for the treatment of neuroblastoma in 2015.|
BEZ235 tosylate is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assay...
GNE-317 is a potent and selective PI3K inhibitor with potential anticncer activity. GNE-317 targets the PI3K pathway and can cross the Blood–Brain Barrier. GNE-...
WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2.
Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM.
AZD-8055 is an inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor AZD8055 inhibits the serine/t...
AZD-3147 is an extremely potent and selective dual inhibitor of mTORC1 and mTORC2. It exhibits >300-fold selectivity for mTOR over PI 3-kinase isoforms. It has ...
mTOR kinase inhibitor OSI-027 is an orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinas...
CZ415 is a highly selective potent mTOR inhibitor with little activity on other lipid and protein kinases with efficacy in a collagen induced arthritis model an...
Dactolisib, also known as BEZ235, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. BEZ235 speci...
MLN0128, also known as INK128, is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR co...
XL PI3K/mTOR inhibitor
An orally bioactive PI3K/mTOR tyrosine kinase inhibitor.
The hydrochloride salt form of CC-115 which is a mTOR / DNA-PK inhibitor that probably has antineoplastic effect through influencing the cellular proliferation ...
CC-115, a DNA-PK and mTOR inhibitor, has been found to have probable anticarcinoma effect. IC50:13 nM and 21 nM for DNA-PK and mTOR respectively.
Omipalisib, also known as GSK2126458, is asmall-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic acti...
DMH-25, a chromene derivative, could be a covalent mTOR inhibitor that has be found to exhibit activity in restraining the growth and metastasis of triple-negat...
Rapamycin is a mTOR inhibitor immunosuppressant and kinase inhibitor with both antifungal and antineoplastic properties. It selectively inhibits the transcripti...
GDC-0084, a PI3K inhibitor, has been found to have probable antineoplastic effect and could pass blood-brain barrier with favourable penetration. It was just li...
Ku-0063794 inhibits both mTORC1 and mTORC2 with an IC50 of approximately 10 nM, but does not suppress the activity of 76 other protein kinases or seven lipid ki...
PQR530 is a potent dual pan PI3K/mTOR inhibitor undergoing phase II clinical trials in 2016. Aberrant activation of the PI3K/mTOR signaling pathway promotes the...
Gedatolisib (PF-05212384, PKI-587)
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2.