Miransertib HCl (ARQ 092; MK-7075)
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $750 | Check With Us |
500mg | $1350 | Check With Us |
1g | $2025 | Check With Us |
Cat #: V3318 CAS #: 1313883-00-9 Purity ≥ 98%
Description: Miransertib HCl (formerly known as ARQ-092; MK7075), the HCl salt of Miransertib, is a novel, orally bioactive and selective allosteric inhibitor of AKT anticancer activity.
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Molecular Weight (MW) | 468.99 |
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Molecular Formula | C27H25ClN6 |
CAS No. | 1313883-00-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: >50 mg/mLr |
Water: N/Ar | |
Ethanol: N/A | |
SMILES Code | NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5.[H]Cl |
Synonyms | ARQ092 hydrochloride; MK-7075; ARQ-092 hydrochloride; MK7075; ARQ 092; 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine hydrochloride |
Protocol | 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). |
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In Vivo | Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinom. 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.1322 mL | 10.6612 mL | 21.3224 mL | 42.6448 mL |
5mM | 0.4264 mL | 2.1322 mL | 4.2645 mL | 8.5290 mL |
10mM | 0.2132 mL | 1.0661 mL | 2.1322 mL | 4.2645 mL |
20mM | 0.1066 mL | 0.5331 mL | 1.0661 mL | 2.1322 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.