HS-10296 hydrochloride | CAT#2134096-03-8 | EGFR inhibitor

MedKoo Cat#: 462530 | Name: HS-10296 hydrochloride

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.

Chemical Structure

HS-10296 hydrochloride

CAS#2134096-03-8

Theoretical Analysis

MedKoo Cat#: 462530

Name: HS-10296 hydrochloride

CAS#: 2134096-03-8

Chemical Formula: C30H36ClN7O2

Exact Mass: 561.2619

Molecular Weight: 562.12

Elemental Analysis: C, 64.10; H, 6.46; Cl, 6.31; N, 17.44; O, 5.69

Price and Availability

Size	Price	Availability
5mg	USD 250.00	2 Weeks
10mg	USD 400.00	2 Weeks
25mg	USD 750.00	2 Weeks

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Synonym

HS-10296 hydrochloride; HS 10296 hydrochloride; HS10296 hydrochloride

IUPAC/Chemical Name

N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide hydrochloride

InChi Key

CUXBWKDZKQGJNN-UHFFFAOYSA-N

InChi Code

InChI=1S/C30H35N7O2.ClH/c1-6-29(38)32-24-17-25(28(39-5)18-27(24)36(4)16-15-35(2)3)34-30-31-14-13-23(33-30)22-19-37(20-11-12-20)26-10-8-7-9-21(22)26;/h6-10,13-14,17-20H,1,11-12,15-16H2,2-5H3,(H,32,38)(H,31,33,34);1H

SMILES Code

COC(C=C(N(C)CCN(C)C)C(NC(C=C)=O)=C1)=C1NC2=NC(C3=CN(C4CC4)C5=C3C=CC=C5)=CC=N2.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM).

In vitro activity:

HS-10296 significantly inhibited the proliferation of MDA-MB-231 cells with IC50 values at 24, 48 and 72 h of 8.393, 2.777 and 2.016 μmol/L, respectively. JC-1 and flow cytometry showed that HS-10296 induced obvious apoptosis of MDA-MB-231 cells, which showed an apoptosis rate of (21.63 ± 2.97)% following treatment with 8 μmol/L HS-10296. Reference: Nan Fang Yi Ke Da Xue Xue Bao. 2020 Jul 30;40(7):981-987. https://pubmed.ncbi.nlm.nih.gov/32895156/

In vivo activity:

Western blotting showed that compared with the control group, the expression levels of MMP-9, MMP-2 and vimentin protein in PC-9 and H1975 cells in 1, 2 and 4 µmol/L almonertinib treatment group were significantly lower, and the expression level of E-cadherin protein was significantly higher (all P<0.05). The experimental results of nude mice showed that compared with the control group and the positive control ositinib (AZD9291) group, the tumor growth was significantly inhibited, the weight of nude mice, the tumor volume and the tumor mass were significantly reduced in the almonertinib treatment group (all P<0.05). Reference: Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Oct 28;46(10):1045-1053. https://pubmed.ncbi.nlm.nih.gov/34911833/

	Solvent	mg/mL	mM
Solubility
	DMSO	83.3	148.24

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 562.12 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhang Y, Zhang Y, Niu W, Ge X, Li X, Fan F, Li S, Liu H. Effect of almonertinib on the proliferation, invasion, and migration in non-small cell lung cancer cells. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Oct 28;46(10):1045-1053. English, Chinese. doi: 10.11817/j.issn.1672-7347.2021.201009. PMID: 34911833. 2. Ge X, Zhou Q, Zhang Y, Zhou W, Wu Y, Zhen C, Zhang M, Fan F, Chen G, Zhao J, Liu H. [EGFR tyrosine kinase inhibitor HS-10296 induces autophagy and apoptosis in triplenegative breast cancer MDA-MB-231 cells]. Nan Fang Yi Ke Da Xue Xue Bao. 2020 Jul 30;40(7):981-987. Chinese. doi: 10.12122/j.issn.1673-4254.2020.07.10. PMID: 32895156; PMCID: PMC7386211.

In vitro protocol:

In vivo protocol:

1: Sullivan I, Planchard D. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne). 2017;3:76. Published 2017 Jan 18. doi:10.3389/fmed.2016.00076 2: Wu SG, Shih JY. Management of acquired resistance to EGFR TKI-targeted therapy in advanced non-small cell lung cancer. Mol Cancer. 2018;17(1):38. Published 2018 Feb 19. doi:10.1186/s12943-018-0777-1