EGFR(表皮生长因子受体)

Cat.No. 产品名称 Information

GC62562 EGFR-IN-11 EGFR-IN-11 是第四代 EGFR-酪氨酸激酶抑制剂 (EGFR-TKI)，对三重突变的 EGFRL858R/T790M/C797S 的 IC50 为 18 nM。EGFR-IN-11 显著抑制 EGFR 磷酸化，诱导细胞凋亡，将细胞周期阻滞在 G0/G1处。

GC62481 AST5902 trimesylate AST5902 is the principal metabolite of alflutinib both in vitro and in vivo, which exerts remarkable antineoplastic activity similar to alflutinib. AST5902 exhibits much weak CYP3A4 induction potential compared to alflutinib.

GC62420 EMI56 EMI56 是 EMI1 的衍生物，EMI56 比 EMI1 对突变型 EGFR 具有更大的效力。EMI56 抑制 EGFR 三重突变体。

GC62402 ASK120067

ASK120067

ASK120067 (ASK120067) 是一种有效的口服活性 EGFRT790M (IC50:0.3 nM) 抑制剂，选择性高于 EGFRWT (IC50:6.0 nM)。 ASK120067是用于非小细胞肺癌（NSCLC）研究的第三代EGFR-TKI。

GC62385 Simotinib Simotinib 是一种选择性、特异性、口服生物利用度高的 EGFR 酪氨酸激酶抑制剂，IC50 为 19.9 nM。抗肿瘤活性。

GC62384 Epitinib succinate

HMPL-813 succinate

Epitinib succinate 是一种具有口服活性和选择性的表皮生长因子受体酪氨酸激酶抑制剂 (EGFR-TKI)，可以透过血脑屏障。Epitinib succinate 可用于癌症研究。

GC62341 Rezivertinib

BPI-7711

Rezivertinib (BPI-7711) 是一种口服有效，高选择性和不可逆的第三代 EGFR 酪氨酸激酶抑制剂 (TKI)。Rezivertinib 对常见的激活 EGFR 和抗性T790M 突变具有高效力。Rezivertinib 具有出色的透过中枢神经系统 (CNS) 能力，并具有抗肿瘤活性。

GC62160 Mobocertinib succinate

莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate

An inhibitor of mutant EGFR and HER2 receptors

GC62159 Tucatinib hemiethanolate

妥卡替尼半乙醇合物,Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate

An inhibitor of HER2

GC61807 (E/Z)-AG490

酪氨酸磷酸化抑制剂AG490,(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42

(E/Z)-AG490((E/Z)-TyrphostinAG490)是(E)-AG490和(Z)-AG490的消旋体。(E)-AG490是一种酪氨酸激酶抑制剂，可抑制EGFR，Stat-3和JAK2/3。

GC61780 SU5204 SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.

GC61490 Trastuzumab emtansine

曲妥珠单抗-美坦新偶联物; Ado-Trastuzumab emtansine; PRO132365; T-DM 1

Trastuzumab Emtansine(T-DM1,Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1.Trastuzumab emtansine has a molecular weight of 145kDa.

GC61473 Trastuzumab deruxtecan

DS-8201 (solution); DS-8201a (solution)

Trastuzumab deruxtecan（曲妥珠单抗）是一种人表皮生长因子受体2（HER2）靶向抗体-药物偶联物（ADC），由人源化抗人HER2（抗hHER2）抗体、酶促裂解肽接头和拓扑异构酶I抑制剂（DX-8951衍生物）组成。

GC50706 JBJ-03-142-02 Highly potent epidermal growth factor receptor (EGFR) and ErbB2 (human epidermal growth factor receptor; HER2) inhibitor

GC47303 Erlotinib-d6 (hydrochloride)

埃罗替尼-D6盐酸盐,CP-358774-d6 hydrochloride; NSC 718781-d6 hydrochloride; OSI-774-d6 hydrochloride

An internal standard for the quantification of erlotinib

GC61161 Osimertinib D6

AZD-9291-d6; Mereletinib-d6

OsimertinibD6(AZD-9291D6)是Osimertinib的一种氘代化合物。Osimertinib是一种不可逆和突变的选择性的EGFR抑制剂，抑制EGFRL858R和EGFRL858R/T790M的IC50分别为12和1nM。

GC60868 Gefitinib D8

吉非替尼杂质-D8,ZD1839-d8

GefitinibD8(ZD1839D8)是Gefitinib的氘代物。Gefitinib是一种有效的(EGFR)抑制剂，在NR6wtEGFR细胞中IC50值为2-37nM。

GC60805 EMI48 EMI48是EMI1的衍生物，EMI48比EMI1对突变型EGFR具有更大的效力。EMI48抑制EGFR三重突变体。

GC60567 Afatinib impurity 11 Afatinib impurity 11 is an impurity of afatinib, an EGFR family inhibitor.

GC60154 Erlotinib D6

CP-358774-d6; NSC 718781-d6; OSI-774-d6

An internal standard for the quantification of erlotinib

GC50083 PKI 166 hydrochloride An inhibitor of EGFR

GC50026 BIBX 1382 dihydrochloride An EGFR inhibitor

GC50013 AG 1478 hydrochloride

N-(3-氯苯基)-6,7-二甲氧基-4-喹唑啉胺盐酸盐,Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride

An inhibitor of EGF receptor kinase

GC38402 BI-4020 BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFRdel19 T790M C797S as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.

GC38350 Epertinib hydrochloride

S-22611 hydrochloride

Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.

GC38180 Cyasterone

杯苋甾酮

Cyasterone，一种天然的 EGFR 抑制剂，主要分离自 Ajuga decumbens Thunb (Labiatae)。Cyasterone 通过诱导细胞凋亡 (apoptosis) 和细胞周期阻滞表现出抗增殖作用。 Cyasterone 可作为抗人类肿瘤的临床治疗性药物。

GC38125 Tyrphostin AG30

酪氨酸磷酸化抑制剂AG30,AG30

Tyrphostin AG30 (AG30), a potent and selective EGFR tyrosine kinase inhibitor, selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.

GC38081 Theliatinib

西利替尼; Xiliertinib; HMPL-309

Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.

GC38006 β-Hydroxyisovalerylshikonin

β-羟基异戊酰基紫草素

Beta-hydroxyisovalerylshikonin 是一种从Lithospermium radix 中分离出的天然产物，是一种有效的 PTK 抑制剂，对 EGFR 和 v-Src 受体作用的 IC50 分别为 0.7 μM 和 1 μM。Beta-hydroxyisovalerylshikonin 对多种肿瘤细胞系均有抑制作用，能高效诱导 NCI-H522 和 DMS114 细胞的死亡。

GC37933 WHI-P180 hydrochloride

Janex 3 hydrochloride;

A multi-kinase inhibitor

GC37568 RTC-5

TRC-382

RTC-5 是一种具有抗癌效力的优化吩噻嗪。RTC-5 显示针对 EGFR 驱动的癌症的异种移植模型的功效，其效果归因于 PI3K-AKT 和 RAS-ERK 信号传导的负调节。

GC36819 Osimertinib dimesylate

奥希替尼二甲磺酸盐; AZD-9291 dimesylate; Mereletinib dimesylate

Osimertinib dimesylate (AZD-9291 dimesylate) 是不可逆的突变体选择性 EGFR 抑制剂；对EGFRL858R 和EGFRL858R/T790M 的 IC50 值分别为12 和 1 nM。

GC36699 Nazartinib mesylate

EGF816 mesylate

An inhibitor of mutant EGFR

GC36667 Mutated EGFR-IN-2 Mutated EGFR-IN-2 (compound 91) 突变选择性的 EGFR 抑制剂，有效抑制单突变体 EGFR (T790M) 和双突变体 EGFR (包括 L858R/T790M (IC50=＜1nM) 和 ex19del/T790M)，并且可以抑制单一功能获得性突变 EGFR (包括 L858R 和 ex19del) 的活性。Mutated EGFR-IN-2 具有抗肿瘤活性。

GC36666 Mutated EGFR-IN-1

AZD9291中间体1,Osimertinib analog

Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.

GC36044 FIIN-3 An inhibitor of FGFRs

GC36003 Erlotinib mesylate

埃罗替尼甲磺酸盐; CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylate

An EGFR tyrosine kinase inhibitor

GC35966 EGFR-IN-7

5-溴-N4-[5-(二甲基膦基)-6-喹喔啉基]-N2-[2-甲氧基-5-甲基-4-[4-(4-甲基-1-哌嗪基)-1-哌啶基]苯基]-2,4-嘧啶二胺

TQB3804 (EGFR-IN-7) is a selective and potent EGFR kinase inhibitor with IC50 of 0.46 nM, 0.13 nM, 0.26 nM, 0.19 nM and 1.07 nM for for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, EGFRL858R/T790M and EGFRWT, respectively. TQB3804 (EGFR-IN-7) shows anti-tumor activity.

GC35965 EGFR mutant-IN-1 EGFR mutant-IN-1 是一种 5-甲基嘧啶吡啶酮衍生物，是有效的，选择性 EGFRL858R/T790M/C797S 突变抑制剂，IC50 为 27.5 nM，对 EGFRWT 的抑制作用明显较低 (IC50 >1.0 μM)。

GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体 (EGFR) 突变型激酶抑制剂，对耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的 IC50 值分别为 5.3 nM 和 8.3 nM。在细胞中，CHMFL-EGFR-202 对 EGFR L858R/T790M 的选择性是 EGFR 野生型的 10 倍。CHMFL-EGFR-202 以 “DFG-in-C-helix-out” 的不活跃结合构象形式共价结合 EGFR，对 EGFR 突变体驱动的非小细胞肺癌 (NSCLC) 细胞株具有较强的抗增殖作用。