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HE3235 is a synthetic adrenal hormone, an androstanediol analog, that functions as an androgen receptor antagonist. It operates in an androgen receptor-dependent manner, downregulating anti-apoptotic genes and upregulating pro-apoptotic genes, which leads to the stimulation of apoptosis. HE3235 has demonstrated its effectiveness in inhibiting androstenediol-dependent LNCaP cell tumor growth in both in vitro (IC50 = 6 nM) and xenograft models in vivo.

183387-50-0

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183387-50-0 Usage

Uses

Used in Pharmaceutical Industry:
HE3235 is used as an androgen receptor antagonist for its ability to inhibit tumor growth in androgen receptor-dependent cancers. Its mechanism of action involves the downregulation of anti-apoptotic genes and the upregulation of pro-apoptotic genes, thereby promoting apoptosis and reducing tumor growth.
Used in Cancer Treatment:
HE3235 is used as a therapeutic agent for the treatment of androgen receptor-dependent cancers. Its effectiveness has been demonstrated in inhibiting LNCaP cell tumor growth, making it a promising candidate for further research and development in cancer treatment.

in vitro

in lncap cells expressing a mutated androgen receptor, he3235 significantly inhibited activity for aed-stimulated lncap proliferation. this inhibitory activity is accompanied by an increase in the number of apoptotic cells [1].

in vivo

animal studies have confirmed the cytoreductive activity of he3235 on lncap tumours. the results suggest that HE3235 may be of clinical use in castration-resistant prostate cancer. in castrated male mice implanted subcutaneously with lucap35v cap xenografts, treatment with he3235 significantly prolonged the tumor doubling time of lucap35v, decreased androgen receptor expression, and lowered levels of intratumoral testosterone by 89% and dihydrotestosterone by 63% in both the presence and the absence of aed. he3235 inhibited tumor growth in the bone environment. he3235 inhibited the growth of subcutaneous crpc as well as crpc in the bone environment. he3235 exhibited a wide range of effects, including alteration of androgen receptor signaling and reductions in levels of intratumoral androgens. weights of tumored tibiae of he3235-treated animals were lower than those of control [3].

references

[1] trauger r, corey e, bell d, et al. inhibition of androstenediol-dependent lncap tumour growth by 17α-ethynyl-5α-androstane-3α, 17β-diol (he3235)[j]. british journal of cancer, 2009, 100(7): 1068-1072.[2] gelmann e p. molecular biology of the androgen receptor[j]. journal of clinical oncology, 2002, 20(13): 3001-3015.[3 gelmann e p. molecular biology of the androgen receptor[j]. journal of clinical oncology, 2002, 20(13): 3001-3015.] koreckij t d, trauger r j, montgomery r b, et al. he3235 inhibits growth of castration-resistant prostate cancer[j]. neoplasia, 2009, 11(11): 1216in22-1225in23.

Check Digit Verification of cas no

The CAS Registry Mumber 183387-50-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,8,3,3,8 and 7 respectively; the second part has 2 digits, 5 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 183387-50:
(8*1)+(7*8)+(6*3)+(5*3)+(4*8)+(3*7)+(2*5)+(1*0)=160
160 % 10 = 0
So 183387-50-0 is a valid CAS Registry Number.

183387-50-0SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 15, 2017

Revision Date: Aug 15, 2017

1.Identification

1.1 GHS Product identifier

Product name (3R,5S,8R,9S,10S,13S,14S,17R)-17-ethynyl-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,14,15,16-tetradecahydrocyclopenta[a]phenanthrene-3,17-diol

1.2 Other means of identification

Product number -
Other names Apoptone

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:183387-50-0 SDS

183387-50-0Upstream product

183387-50-0Downstream Products

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