Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9997 |
GLL 398
|
Estrogen Receptor/ERR | Endocrinology/Hormones |
GLL 398 是一种具有口服活性的选择性雌激素受体降解剂,IC50 为 1.14 nM。 GLL 398 在异种移植乳腺癌模型中阻断肿瘤生长。 | |||
T5118 |
Brilanestrant
GDC0810,GDC 0810,GDC-0810,ARN-810,RG 6046 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
Brilanestrant (GDC-0810) 是一种雌激素选择性降能器 (selective estrogen receptor degrader)(IC50:0.7 nM),口服具有活性。 | |||
T39727 |
ERα degrader-2
|
ERK | MAPK |
ERα degrader-2 是一种具有选择性和有效性的雌激素受体 (SERD)降解剂,具有抗癌活性,抑制 ERα,对雌激素受体降解的 EC50 值为 0.3 nM。ERα degrader-2 可用于预防和治疗 HER 阳性乳腺癌。 | |||
T15788 |
LSZ-102
LSZ102 |
Estrogen Receptor/ERR | Endocrinology/Hormones |
LSZ-102是一种有效和选择性的雌激素受体降解剂(IC50 = 0.2 nM),可用于有关ERα阳性乳腺癌的研究。 | |||
T13674 |
Elacestrant
依拉司群,RAD1901 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
Elacestrant (RAD1901) 是一种具有口服活性的、选择性的雌激素受体 (ER) 降解剂 (SERD),能够作用于 ERα (IC50:48 nM)和 ERβ (IC50:870 nM)。 | |||
T13675 |
Elacestrant dihydrochloride
RAD1901 dihydrochloride |
Estrogen/progestogen Receptor | Endocrinology/Hormones |
Elacestrant dihydrochloride (DA-DKRAD1901 dihydrochloride) 是一种具有口服活性的的选择性雌激素受体 (ER) 降解剂 (SERD),能够作用于 ERα (IC50:48 nM) 和 ERβ (IC50:870 nM)。 | |||
T12832 |
Amcenestrant
SAR439859 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
Amcenestrant (SAR439859) 是一种有效的 ER 拮抗剂,具有 ER 降解活性,EC50为 0.2 nM。它是一种具有口服活性,非甾体和选择性雌激素受体降解剂 (SERD)。它可在 ER+乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。 | |||
T39499 |
Rintodestrant
G1T48 |
||
Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) that also functions as a CDK4/6 inhibitor. | |||
T39118 |
AZD9496 maleate
|
||
AZD9496 maleate is a highly potent and selective antagonist of the estrogen receptor alpha (ERα), exhibiting an IC50 value of 0.28 nM. This compound, AZD9496 maleate, is an orally bioavailable selective estrogen receptor degrader (SERD). | |||
T70179 |
THIQ-40
|
||
THIQ-40 is a novel potent erα antagonist and selective estrogen receptor degrader (serd), exhibiting good oral bioavailability, antitumor efficacy, and serd activity in vivo | |||
T63922 | ERα degrader 5 | ||
ERα degrader 5 是一种口服具有活力的、选择性的雌激素受体 (estrogen receptor (ER)) 降解剂,能够作用于 ERα (EC50: 1.1 nM)。ERα degrader 5 在体内显示抗肿瘤效果。 | |||
T74856 | ER degrader 4 | ||
ER degrader 4,一种选择性且口服活性的雌激素受体(estrogen receptor)降解剂,展现出抗肿瘤活性。 | |||
T39368 | GNE-149 | ||
GNE-149 is an orally bioavailable compound that acts as a full antagonist of estrogen receptor α (ERα) with an IC50 of 0.053 nM. It is also classified as a selective estrogen receptor degrader (SERD). GNE-149 holds potential for research in the field of breast cancer. | |||
T11173 |
Elacestrant S enantiomer
RAD1901 S enantiomer |
Others | Others |
Elacestrant S enantiomer is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. | |||
T63674 |
Imlunestrant
|
||
Imlunestrant 是选择性的、口服具有活力的雌激素受体的降解剂(SERD),能够用于 ER+ 和HER2 乳腺癌的研究。 | |||
T11173L |
Elacestrant S enantiomer dihydrochloride
RAD1901 S enantiomer dihydrochloride,RAD-1901 S enantiomer dihydrochloride,RAD 1901 S enantiomer dihydrochloride |
Others | Others |
Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant S enantiomer dihydrochloride is an low activity enantiomer of elacestrant dihydrochloride. | |||
T79382 |
ER degrader 6
|
Estrogen Receptor/ERR | Endocrinology/Hormones |
ER degrader 6 (compound 35s) 是高效的雌激素受体 (ER)α降解剂,作用机制为通过抑制微管蛋白聚合破坏微管网络。该化合物能抑制肿瘤生长,并展现出较低的毒性特性。 | |||
T74593 | Taragarestrant meglumine | ||
Taragarestrant meglumine (D-0502) 是一种口服有效、选择性的雌激素受体 (estrogen receptor) 降解剂,展现了对各种ER+乳腺癌细胞系及移植模型的强大活性。 | |||
T74415 | Imlunestrant tosylate | ||
Imlunestrant (LY-3484356) tosylate 是口服有效且选择性的雌激素受体(estrogen receptor, ER)降解剂(SERD),具纯拮抗性。该化合物能持续抑制ER依赖的基因转录与细胞生长,适用于研究ER阳性(ER+)晚期乳腺癌(aBC)与子宫内膜样癌(EEC)。 | |||
T63165 | LX-039 | ||
LX-039 是一种高效的、选择性的、口服具有活力的雌激素受体降解剂 (EC50: 2.99 nM),具有抗肿瘤作用。LX-039 有吲哚 C-3 氯原子。LX-039 具有良好的小鼠药代动力学性质、低清除、高血药浓度和口服暴露率。 |