Name: Sapanisertib (MLN0128, INK-128)
Brand: Selleck Chemicals
SKU: S2811
Rating: 5 (131 reviews)

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.94%

99.94

Verwandte Ziele	PI3K Akt GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PI4K PP2A
Weitere mTOR Inhibitoren	Torin 1 Torin 2 AZD8055 Ridaforolimus (Deforolimus, MK-8669) Torkinib (PP242) MHY1485 Vistusertib (AZD2014) KU-0063794 OSI-027 3BDO

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	PMID
U87	Function assay			Inhibition of mTOR in human U87 cells assessed as reduction in p4EBP1 phosphorylation by Western blot method	ChEMBL
U87	Function assay			Inhibition of mTOR in human U87 cells assessed as reduction in pAKT phosphorylation at residue 47 by Western blot method	ChEMBL
PC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC3 cells measured after 72 hrs by Alamar blue dye-based fluorescence analysis, EC50 = 0.1 μM.	ChEMBL
SKOV3	Function assay		1 hr	Inhibition of TORC2 in human SKOV3 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis	30359003
A2058	Function assay		1 hr	Inhibition of TORC1 in human A2058 cells assessed as decrease in S6K phosphorylation after 1 hr by Western blot analysis	30359003
SKOV3	Function assay		1 hr	Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6K phosphorylation after 1 hr by Western blot analysis	30359003
SKOV3	Function assay		1 hr	Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis	30359003
SKOV3	Function assay		1 hr	Inhibition of TORC1 in human SKOV3 cells assessed as decrease in 4E-BP1 phosphorylation after 1 hr by Western blot analysis	30359003
A2058	Function assay		1 hr	Inhibition of TORC1 in human A2058 cells assessed as decrease in 4E-BP1 phosphorylation after 1 hr by Western blot analysis	30359003
A2058	Function assay		1 hr	Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis	30359003
A2058	Function assay		1 hr	Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis	30359003
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
PANC-1	Cell Viability Assay	1-100 nM	72 h	inhibits cell viability dose dependently	24971544
PANC-1	Cell Viability Assay	50 nM	24-96 h	inhibits cell viability time dependently	24971544
MIA PaCa-2	Cell Viability Assay	1-100 nM	72 h	inhibits cell viability dose dependently	24971544
PANC-1	Apoptosis Assay	10-100 nM	72 h	induces apoptosis dose dependently	24971544
PANC-1	Function Assay	10/50 nM	24 h	dramatically inhibits phosphorylation of 4E-BP1-S6K1 (mTORC1 activation indicators) and Akt at Ser 473 (the mTORC2 activation indicator)	24971544
PANC-1	Function Assay	10 nM	72 h	increases LY 188011 sensitivity	24971544
PANC-1	Function Assay	50 nM	48 h	disrupts cell cycle progression	24971544
U87	Function assay			Inhibition of mTOR pS6K in human U87 cells assessed as inhibition of 4EBP1 phosphorylation by Western blot analysis	ChEMBL
U87	Function assay			Inhibition of mTOR in human U87 cells assessed as reduction in pRAS40 phosphorylation by Western blot method	ChEMBL
U87	Function assay			Inhibition of mTOR pS6K in human U87 cells assessed as inhibition of RAS40 phosphorylation by Western blot analysis	ChEMBL
U87	Antitumor assay	0.3 to 3 mg/kg	14 days	Antitumor activity against human U87 cells xenografted in mouse assessed as tumor growth inhibition at 0.3 to 3 mg/kg measured after 14 days	ChEMBL
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht	309.33	Formel	C₁₅H₁₅N₇O	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	1224844-38-5	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	INK 128,TAK-228			Smiles	CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 62 mg/mL (200.43 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

DMSO : 62 mg/mL (200.43 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 62 mg/mL (200.43 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 62 mg/mL (200.43 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Targets/IC₅₀/Ki	mTOR (Cell-free assay) 1.4 nM(Ki) mTOR (Cell-free assay) 1.4 nM(Ki) PI3Kα (Cell-free assay) 219 nM PI3Kγ (Cell-free assay) 221 nM PI3Kδ (Cell-free assay) 230 nM PI3Kβ (Cell-free assay) 5293 nM
In vitro	INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. 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.
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. Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/20622997/ [2] http://mct.aacrjournals.org/cgi/content/meeting_abstract/8/12_MeetingAbstracts/B148 [3] https://pubmed.ncbi.nlm.nih.gov/22367541/

Anwendungen (Applications)

Methoden	Biomarker	Bilder	PMID
Western blot	p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt CD44 / Vimentin c-Jun p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6 FKBP1 / MARS / CDC25A / TCL1A		25425103
Growth inhibition assay	Cell viability		25425103

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2026-07-02)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
NCT07558733	RECRUITING	HR+ HER2- Breast Cancer	Faeth Therapeutics	2026-04-22	PHASE1; PHASE2
NCT06463028	RECRUITING	Endometrial Cancer	Faeth Therapeutics	2024-12-12	PHASE2
NCT06811116	RECRUITING	Advanced Hepatocellular Carcinoma; Metastatic Hepatocellular Carcinoma; Stage III Hepatocellular Carcinoma AJCC v8; Stage IV Hepatocellular Carcinoma AJCC v8	National Cancer Institute (NCI)	2025-11-17	PHASE1; PHASE2
NCT02503722	ACTIVE_NOT_RECRUITING	Metastatic Lung Non-Small Cell Carcinoma; Recurrent Lung Non-Small Cell Carcinoma; Stage III Lung Non-Small Cell Cancer AJCC v7; Stage IIIA Lung Non-Small Cell Cancer AJCC v7; Stage IIIB Lung Non-Small Cell Cancer AJCC v7; Stage IV Lung Non-Small Cell Cancer AJCC v7	National Cancer Institute (NCI)	2017-03-23	PHASE1
NCT02465060	ACTIVE_NOT_RECRUITING	Advanced Lymphoma; Advanced Malignant Solid Neoplasm; Bladder Carcinoma; Breast Carcinoma; Cervical Carcinoma; Colon Carcinoma; Colorectal Carcinoma; Endometrial Carcinoma; Esophageal Carcinoma; Exocrine Pancreas Carcinoma; Gastric Carcinoma; Glioma; Head and Neck Carcinoma; Hematopoietic and Lymphoid Cell Neoplasm; Kidney Carcinoma; Liver Carcinoma; Lung Carcinoma; Lymphoma; Malignant Uterine Corpus Neoplasm; Malignant Uterine Neoplasm; Melanoma; Multiple Myeloma; Ovarian Carcinoma; Prostate Carcinoma; Rectal Carcinoma; Recurrent Bladder Carcinoma; Recurrent Breast Carcinoma; Recurrent Cervical Carcinoma; Recurrent Colon Carcinoma; Recurrent Colorectal Carcinoma; Recurrent Esophageal Carcinoma; Recurrent Gastric Carcinoma; Recurrent Glioma; Recurrent Head and Neck Carcinoma; Recurrent Liver Carcinoma; Recurrent Lung Carcinoma; Recurrent Lymphoma; Recurrent Malignant Solid Neoplasm; Recurrent Malignant Uterine Corpus Neoplasm; Recurrent Melanoma; Recurrent Multiple Myeloma; Recurrent Ovarian Carcinoma; Recurrent Pancreatic Carcinoma; Recurrent Prostate Carcinoma; Recurrent Rectal Carcinoma; Recurrent Skin Carcinoma; Recurrent Thyroid Gland Carcinoma; Refractory Lymphoma; Refractory Malignant Solid Neoplasm; Refractory Multiple Myeloma; Skin Carcinoma; Thyroid Gland Carcinoma	National Cancer Institute (NCI)	2015-08-17	PHASE2
NCT06390865	ACTIVE_NOT_RECRUITING	Advanced Lymphoma; Advanced Malignant Solid Neoplasm; Refractory Lymphoma; Refractory Malignant Solid Neoplasm; Refractory Multiple Myeloma	National Cancer Institute (NCI)	2017-03-12	PHASE2

Häufig gestellte Fragen (Frequently Asked Questions)

Frage 1:
What is the recommendation method to formulate it for oral administration?

Antwort:
For oral administration, it can be tried with this vehicle: 30% PEG400+0.5% Tween80 +5% Propylene glycol.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Sapanisertib (MLN0128, INK-128) mTOR Inhibitor

Molekulargewicht: 309.33

Qualitätskontrolle (Quality Control)

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Löslichkeit (Solubility)

Molaritätsrechner

In-vivo-Formulierungsrechner (Klare Lösung)

Wirkmechanismus (Mechanism of Action)

Anwendungen (Applications)

Klinische Studieninformationen (Clinical Trial Information)

Häufig gestellte Fragen (Frequently Asked Questions)

Sapanisertib (MLN0128, INK-128) mTOR Inhibitor

Molekulargewicht: 309.33

Qualitätskontrolle (Quality Control)

Zellkultur, Behandlung & Arbeitskonzentration (Cell Culture, Treatment & Working Concentration)

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Löslichkeit (Solubility)

Molaritätsrechner

In-vivo-Formulierungsrechner (Klare Lösung)

Wirkmechanismus (Mechanism of Action)

Anwendungen (Applications)

Klinische Studieninformationen (Clinical Trial Information)

Häufig gestellte Fragen (Frequently Asked Questions)

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)