Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T21761 |
HNMPA
|
IGF-1R | Tyrosine Kinase/Adaptors |
HNMPA 是膜不可渗透的胰岛素受体酪氨酸激酶 (insulin receptor tyrosine kinase) 抑制剂。HNMPA 可以抑制人胰岛素受体的酪氨酸和丝氨酸自磷酸化。HNMPA 对环 AMP 依赖性蛋白激酶或蛋白激酶 C 活性没有影响。 | |||
T36287 |
Pirtobrutinib
|
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrat... | |||
T38562 |
AKN-028
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
AKN-028 是酪氨酸激酶 FLT3的抑制剂,可剂量依赖性的诱导 FLT3的自磷酸化。 | |||
T7673 |
ATH686
ATH 686 |
Apoptosis; FLT | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
ATH686 是一种选择性的,ATP 竞争性的FLT3抑制剂,具有抗白血病作用。它靶向突变 FLT3 蛋白激酶活性,并通过诱导凋亡和抑制细胞周期来抑制具有 FLT3 突变的细胞的增殖。 | |||
T5168 |
EGFR-IN-12
EGFR Inhibitor |
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-12 (EGFR Inhibitor) 是一种 4,6-二取代的嘧啶,可诱导细胞凋亡,具有抗肿瘤活性。它是ATP 竞争性,不可逆且高度选择性的EGFR 抑制剂,IC50为 21 nM。它对EGFR 的选择性高于 HER4 和 55种其他激酶。它还抑制突变型EGFRL858R 和EGFRL861Q,IC50分别为 63 nM 和 4 nM。 | |||
T2655 |
CEP-37440
CEP37440 |
FAK; ALK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
CEP-37440 是一种新型的 FAK (IC50:2.3 nM) 和 ALK (IC50:120 nM) 双重抑制剂。 | |||
T23127 |
PD-161570
PD 161570 |
EGFR; FGFR; PDGFR; Src | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
PD-161570 是一种有效的 ATP 竞争性人 FGF-1 受体抑制剂,IC50 为 39.9 nM,Ki 为 42 nM。它还是骨形态发生蛋白 (BMPs) 和TGF-β信号抑制剂。它抑制PDGF 刺激的自磷酸化和FGF-1受体磷酸化,IC50分别为 450 和 622 nM。它抑制 PDGFR、EGFR 和 c-Src 酪氨酸激酶,IC50 值分别为 310、240 和 44 nM。 | |||
T1667 |
Tandutinib
MLN518,CT53518,NSC726292,坦度替尼 |
Apoptosis; FLT; CSF-1R; PDGFR; Src; c-Kit | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
Tandutinib (CT53518) 是一种选择性 FLT3抑制剂,其 IC50为 0.22 μM。它还抑制c-Kit 和PDGFR,其IC50分别为 0.17 μM 和 0.20 μM。它可穿透血脑屏障,用于急性骨髓性白血病。 | |||
T14137 |
AG 1295
|
PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
AG 1295 是选择性血小板衍生生长因子受体酪氨酸激酶抑制剂。它能抑制 PDGFR 的自磷酸化,对 EGF 受体的自磷酸化无影响。 | |||
T3545 |
RG13022
RG 13022,Tyrphostin RG13022 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
RG13022 (Tyrphostin RG13022) 是一种酪氨酸激酶抑制剂,抑制EGF 受体自身磷酸化的IC50值为4 μM。 | |||
T3691 |
(Rac)-SAR131675
SAR131675 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
(Rac)-SAR131675 是一种有效的、选择性的VEGFR3抑制剂,其IC50=23 nM。 | |||
T22462 | 1,2,3,4,5,6-Hexabromocyclohexane | Others | Others |
The compound effectively and directly inhibits JAK2 tyrosine kinase autophosphorylation and specifically inhibits ligand-dependent JAK2 activation. It has no cytotoxicity at 100 μM. A 16-hour treatment with compound (1 μM) decreases JAK2 tyrosine autophos | |||
T69863 | Dihydrogenistein | ||
Dihydrogenistein is a derivative of Genistein -- a compound that exhibits specific inhibitory activity against tyrosine kinases including autophosphorylation of epidermal growth factor receptor kinase. | |||
T69260 |
Genistein Diglucuronide
|
||
Genistein Diglucuronide is a metabolite of Genistein which exhibits specific inhibitory activity against tyrosine kinases including autophosphorylation of epidermal growth factor receptor kinase. | |||
T12610L |
3-Hydroxy Midostaurin
CGP52421 |
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412[1]. | |||
T19119 |
3-Hydroxy Midostaurin-D5
CGP52421-D5 |
Others | Others |
3-Hydroxy Midostaurin-D5 (CGP52421-D5) is a deuterium-labeled 3-Hydroxy Midostaurin which is a metabolite of PKC412. PKC412 effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation (IC50s: 132 nM and 9.8 μM in culture medium and plasma). | |||
T40785 |
Gefitinib impurity 1
|
||
Gefitinib impurity 1 is a compound derived from Gefitinib, a potent and selective EGFR tyrosine kinase inhibitor (IC 50 = 33 nM). This orally active compound selectively inhibits tumor cell growth stimulated by EGF (IC 50 = 54 nM) and inhibits EGFR autophosphorylation induced by EGF in tumor cells. Additionally, Gefitinib induces autophagy and exhibits antitumor activity. | |||
T76019 |
[pTyr5] EGFR (988-993) (TFA)
|
||
[pTyr5]EGFR(988-993) TFA 来源于表皮生长因子受体 (EGFR 988-993) 的自磷酸化位点 (Tyr992)。[pTyr5] EGFR(988-993) TFA 常与催化活性低的蛋白-酪氨酸磷酸1B (PTP1B) 结合。 | |||
T70444 |
Edicotinib HCl
|
||
Edicotinib, also known as JNJ-40346527, is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between FMS and its ligand CSF1, thereby preventing autophosphorylation of FMS. As a result, unphosphorylated FMS cannot activate FMS-mediated signaling pathways, thus potentially inhibiting cell proliferation in FMS-overexpressed tum... | |||
T1181L |
Gefitinib hydrochloride
|
||
Gefitinib hydrochloride (ZD1839 hydrochloride) 是一种有效,选择性和具有口服活性的EGFR 酪氨酸激酶抑制剂,IC50为 33 nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50为 54 nM),并阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib hydrochloride 也诱导细胞自噬 (autophagy),具有抗肿瘤活性。 | |||
T61358 |
AKN-028 acetate
|
||
AKN-028 acetate 是一种新型酪氨酸激酶 (TKI) 抑制剂,是一种有效的口服活性的 FMS 样受体酪氨酸激酶 3 (FLT3) 抑制剂,其 IC50值为 6 nM。AKN-028 acetate 抑制 FLT3 自磷酸化。AKN-028 acetate 诱导剂量依赖性的细胞毒性反应 (平均IC50=1 μM)。AKN-028 acetate 通过激活 caspase 3 诱导细胞凋亡 (apoptosis)。AKN-028 acetate 可用于急性髓系白血病 (AML) 的研究。 | |||
T63630 |
Gefitinib dihydrochloride
|
||
Gefitinib dihydrochloride 是有效的、选择性的、口服具有活力的 EGFR 酪氨酸激酶抑制剂 (IC50: 33 nM)。Gefitinib dihydrochloride 能够选择性抑制 EGF 刺激的肿瘤细胞生长,其IC50值为 54 nM,能够阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib dihydrochloride 可以诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),能够用于进行癌症相关疾病,如肺癌和乳腺癌的研究。 | |||
T35915 |
Erlotinib-13C6
Erlotinib-13C6 |
||
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]... | |||
T68389 | LY2457546 | ||
LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 synge... | |||
T67442 |
CGP-53716
|
||
The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smoo... |