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Miransertib

CAT: 0013-GTR19163874-02Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163874-02Size:5 mg
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Description
Miransertib (ARQ-092) is a potent, selective and allosteric inhibitor of Akt1/2/3 with IC50 of 5/4.5/16 nM respectively; inhibits cellular AKT activation and the phosphorylation of the downstream target PRAS40; inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma; orally bioavailable.Blood Cancer Phase 1 Clinical (In Vitro) :In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells. The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC50=0.31 μM) .Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis-infected macrophages. Miransertib also enhances mTOR dependent autophagy in Leishmania-infected macrophages (In Vivo) :Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t1/2 values of 17 h in rats versus 7 h in monkeys. The Cmax is 198 ng/mL and 258 ng/mL and the AUCinf was 5496 h ng/mL and 2960 h ng/mL in rats and monkeys, respectively.Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.
CAS Number
1313881-70-7
Product Name Alternative
ARQ-092
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 40.2 mg/mL
Smiles
C1CC (C1) (C2=CC=C (C=C2) N3C4=C (C=CC (=N4) C5=CC=CC=C5) N=C3C6=C (N=CC=C6) N) N
Molecular Formula
C27H24N6
Molecular Weight
432.5197
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Pyridinamine, 3-[3-[4- (1-aminocyclobutyl) phenyl]-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl]-

Chemical Information

Miransertib

Miransertib is under investigation in clinical trial NCT01473095 (Phase 1 Dose Escalation Study of ARQ 092 in Adult Subjects With Advanced Solid Tumors and Recurrent Malignant Lymphoma).

CAS Number1313881-70-7
PubChem CID53262401
IUPAC Name3-[3-[4-(1-aminocyclobutyl)phenyl]-5-phenylimidazo[4,5-b]pyridin-2-yl]pyridin-2-amine
Molecular FormulaC27H24N6
Molecular Weight432.5
XLogP3.8
Topological Polar Surface Area95.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count4
Heavy Atom Count33
Formal Charge0
Complexity653
SMILES
C1CC(C1)(C2=CC=C(C=C2)N3C4=C(C=CC(=N4)C5=CC=CC=C5)N=C3C6=C(N=CC=C6)N)N
InChI
InChI=1S/C27H24N6/c28-24-21(8-4-17-30-24)25-32-23-14-13-22(18-6-2-1-3-7-18)31-26(23)33(25)20-11-9-19(10-12-20)27(29)15-5-16-27/h1-4,6-14,17H,5,15-16,29H2,(H2,28,30)
InChIKey
HNFMVVHMKGFCMB-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Miransertib
CAS: 1313881-70-7
CID: 53262401
Formula: C27H24N6
MW: 432.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight432.5
XLogP33.8
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count4
Exact Mass432.20624479
Monoisotopic Mass432.20624479
Topological Polar Surface Area95.6 Ų
Heavy Atom Count33
Formal Charge0
Complexity653
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
C8430-1Miransertib
T22247-01Miransertib hydrochloride
207082Miransertib HCl
T70152-01Miransertib mesylate
HY-19719A-01Miransertib (hydrochloride)
A22376-25Miransertib hydrochloride 25mg
A22376-10Miransertib hydrochloride 10mg
C12232-5mgMiransertib (ARQ-092)
A22376-5Miransertib hydrochloride 5mg
A22376-1Miransertib hydrochloride 1mg

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