Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5402 |
DDR1-IN-2
DDR1 inhibitor 7rh |
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
DDR1-IN-2 (DDR1 inhibitor 7rh) 是盘状结构域受体 1 抑制剂 (IC50:13.1 nM),对 DDR2 的抑制作用相对较弱 (IC50:203 nM)。 | |||
T3337 |
Ddr1-In-1
|
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
DDR1-IN-1 是一种特异性的 DDR1 受体酪氨酸激酶抑制剂,选择性是 DDR2 的 3 倍左右。 | |||
T40061 |
DDR1-IN-6
DDR1-IN-6 |
||
DDR1-IN-6 is a potent and selective inhibitor of Discoidin Domain Receptor family member 1 (DDR1), exhibiting remarkable inhibitory activity at an IC50 of 9.72 nM. It effectively suppresses the auto-phosphorylation of DDR1b (Y513) with an IC50 value of 9.7 nM. Furthermore, DDR1-IN-6 displays strong anti-cancer activity. | |||
T40062 |
DDR1-IN-5
DDR1-IN-5 |
||
DDR1-IN-5 is a potent and selective inhibitor of the Discoidin Domain Receptor family, member 1 (DDR1). It effectively inhibits the phosphorylation of DDR1b (Y513) with an IC 50 value of 4.1 nM. Furthermore, DDR1-IN-5 demonstrates remarkable anti-cancer activity. Its inhibitory potency against DDR1 (IC 50 = 7.36 nM) makes it a promising compound for targeted therapy in cancer treatment. | |||
T39572 |
DDR1-IN-4
DDR1-IN-4 |
||
DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation. This compound demonstrates exceptional efficacy with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively. | |||
T70202 |
DDR1-IN-1 dihydrochloride
|
||
DDR1-IN-1 dihydrochloride 是 DDR1受体酪氨酸激酶抑制剂,IC50值为105 nM,而对 DDR2的 IC50为413 nM。 | |||
T79811 |
DDR1/2 inhibitor-2
|
||
DDR1/2 inhibitor-2 (Example 31),作为一种DDR1/DDR2抑制剂,其IC50值小于100 nM,适用于癌症和纤维化疾病的研究领域。 | |||
T70201 |
S 16020-2
|
||
S 16020-2 is an olivacine derivative, and DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors. | |||
T4646 |
TA-02
|
p38 MAPK; Autophagy | Autophagy; MAPK |
TA02 是一种Adezmapimod 类似物,是p38 MAPK 的抑制剂,其IC50值为 20 nM。它和Adezmapimod、SB 202190 具有相似的心源活性,可抑制 TGFBR-2。 | |||
T4349 |
Sitravatinib
MG516,MGCD516 |
Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。 | |||
T10984 |
DDR-TRK-1
|
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
DDR-TRK-1 是 DDR1的一个选择性抑制剂,其 IC50 值为 9.4 nM。DDR-TRK-1 也抑制 TRK 激酶家族。 | |||
T7862 |
VU6015929
|
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
VU6015929 是一种活性双盘状结构域受体 1/2 (DDR1/2) 的抑制剂(IC50 分别为 4.67 nM 和 7.39 nM)。 | |||
T10985 |
DDR Inhibitor
|
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
DDR Inhibitor 是一种高效的盘状结构域受体 (discoidin domain receptor) 抑制剂,对 DDR2 的 IC50 值为 3.3 nM,在浓度为 1.5 nM 时,对 DDR1 有 53% 的抑制作用。 | |||
T12925 |
Sitravatinib malate
MGCD516 malate,MG-516 malate |
TAM Receptor | Tyrosine Kinase/Adaptors |
Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment. | |||
T60805 | JNK3 inhibitor-2 | ||
JNK3 inhibitor-2 是一种有效的选择性JNK3抑制剂。JNK3 inhibitor-2 对 JNK1、JNK2、 JNK3的IC50值分别为 >100, >100, 0.25 μM。JNK3 inhibitor-2也抑制 DDR1 和 EGFR (T790M, L858R)。 | |||
T15808 |
Merestinib dihydrochloride
LY2801653 dihydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), RO | |||
T10801 |
CHMFL-ABL/KIT-155
CHMFL-ABL-KIT-155 |
c-Kit | Tyrosine Kinase/Adaptors |
CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis. |