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Sapanisertib (MLN0128)

Sapanisertib (MLN0128)

Item no.	S2811-5
Manufacturer	Selleckchem
CASRN	1224844-38-5
Amount	5 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer Lymphatic System Cancer
Type	Inhibitors
Specific against	other
Smiles	CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	INK 128,TAK-228
Similar products	INK
Available
Manufacturer - Targets	MTOR
Storage Conditions	2 years -80 in solvent
Molecular Weight	309, 33
Clinical Trials	INK 128 is currently in Phase I clinical trials in patients with relapsed or refractory multiple myeloma or waldenstrom macroglobulinemia.
IC50	1 nM [1], 1 nM [1], 1 nM [1], 1 nM [1], 1 nM [1], 1 nM [1]
In vitro	INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. [1] As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors. [2]
In vivo	In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. [1] Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models. [2]
Solubility (25C)	DMSO 62 mg/mL, Water <1 mg/mL, Ethanol 2 mg/mL
Information	Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Chemical Name	3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3, 4-d]pyrimidin-4-amine

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S2811-5-datasheet.pdf

S2811-5-safety-datasheet.pdf