INY-03-041 trihydrochloride

Name: INY-03-041 trihydrochloride
Brand: MedChemExpress
SKU: HY-133120A
Rating: 4.5 (1 reviews)

Cat. No.: HY-133120A Purity: 99.27%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively.

For research use only. We do not sell to patients.

INY-03-041 trihydrochloride Chemical Structure

Size	Price	Stock	Quantity
1 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1750	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 2800	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of INY-03-041 trihydrochloride:

INY-03-041 Get quote

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Akt Isoform Specific Products:

View All Isoforms

Akt Akt1 Akt2 Akt3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Akt1

2.0 nM (IC₅₀)

Akt3

3.5 nM (IC₅₀)

Akt2

6.8 nM (IC₅₀)

Cereblon

In Vitro

INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells^[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC₅₀ =37.3 nM) and PKG1 (IC₅₀ = 33.2 nM)^[1].
INY-03-041 displays enhanced anti-proliferative effects compared with Ipatasertib (HY-15186) in MDA-MB-468 and HCC1937 cells^[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-468 cells
Concentration:	0, 10, 50, 100, 250, 500, and 1000 nM
Incubation Time:	0, 2, 4, 6, 8. 10, 12, and 24 h
Result:	Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h.

Molecular Weight

907.80

Formula

C₄₄H₅₉Cl₄N₇O₅

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C(N(CC1=C2C=CC=C1CCCCCCCCCCNC[C@H](C3=CC=C(Cl)C=C3)C(N4CCN(C5=C([C@H](C)C[C@H]6O)C6=NC=N5)CC4)=O)C2=O)CC7)NC7=O.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 140 mg/mL (154.22 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1016 mL	5.5078 mL	11.0156 mL
5 mM	0.2203 mL	1.1016 mL	2.2031 mL
10 mM	0.1102 mL	0.5508 mL	1.1016 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.27%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (247 KB) HNMR (252 KB) RP-HPLC (242 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. You I, et al. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7. [Content Brief]

[2]. Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther. 2012 Feb;11(2):317-28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.1016 mL	5.5078 mL	11.0156 mL	27.5391 mL
	5 mM	0.2203 mL	1.1016 mL	2.2031 mL	5.5078 mL
	10 mM	0.1102 mL	0.5508 mL	1.1016 mL	2.7539 mL
	15 mM	0.0734 mL	0.3672 mL	0.7344 mL	1.8359 mL
	20 mM	0.0551 mL	0.2754 mL	0.5508 mL	1.3770 mL
	25 mM	0.0441 mL	0.2203 mL	0.4406 mL	1.1016 mL
	30 mM	0.0367 mL	0.1836 mL	0.3672 mL	0.9180 mL
	40 mM	0.0275 mL	0.1377 mL	0.2754 mL	0.6885 mL
	50 mM	0.0220 mL	0.1102 mL	0.2203 mL	0.5508 mL
	60 mM	0.0184 mL	0.0918 mL	0.1836 mL	0.4590 mL
	80 mM	0.0138 mL	0.0688 mL	0.1377 mL	0.3442 mL
	100 mM	0.0110 mL	0.0551 mL	0.1102 mL	0.2754 mL