Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3196 |
GNF-7
GNF7 |
Bcr-Abl; ACK; AChR | Angiogenesis; Cytoskeletal Signaling; Neuroscience; Tyrosine Kinase/Adaptors |
GNF-7 是一种多重激酶抑制剂。它对ACK1和GCK 具有抑制活性,IC50分别为 25 nM 和 8 nM。它是一种 Bcr-Abl 的抑制剂,对 Bcr-AblWT 和 Bcr-AblT315I 作用的IC50值分别为 133 nM 和 61 nM。它可用于研究血液恶性肿瘤。 | |||
T3071 |
Olverembatinib
GZD 824 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Olverembatinib (GZD 824) 是一种高效的、口服具有活性的pan-Bcr-Abl 抑制剂,具有抗肿瘤活性。它能广泛而有效地抑制突变型 Bcr-Abl。它对天然的 Bcr-Abl 和 Bcr-AblT315I 作用的IC50值分别为 0.34 nM 和 0.68 nM。 | |||
T2429 |
Olverembatinib dimesylate
GZD824 Dimesylate,HQP1351 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Olverembatinib dimesylate (GZD824 Dimesylate) 是一种高效的、口服具有活性的pan-Bcr-Abl 抑制剂,具有抗肿瘤活性。它能广泛而有效地抑制突变型 Bcr-Abl。它对天然的 Bcr-Abl 和 Bcr-AblT315I 作用的IC50值分别为 0.34 nM 和 0.68 nM。 | |||
T10800 |
CHMFL-ABL-121
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
CHMFL-ABL-121 是一种 II 型 ABL 激酶高效抑制剂,抑制纯化的非活性 ABL wt 和 T315I 激酶蛋白的 IC50 值分别为 2 nM 和 0.2 nM。 | |||
T4618 |
BGG463
K 0859 |
Bcr-Abl; CDK | Angiogenesis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
BGG463 (K 0859) 是一种具有口服活性的 II 型 CDK2的抑制剂,可抑制 c-ABL-T334I、BCR-ABL 和 BCR-ABL-T315I 变体,IC50分别为 0.25 μM、0.09 μM 和 0.590 μM。 | |||
T72958 |
BCR-ABL-IN-7
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
BCR-ABL-IN-7 是一种 WT 和 T315I 突变体 ABL 激酶抑制剂。BCR-ABL-IN-7 有效抑制 WT 和 T315I 突变体 ABL 激酶的活性。BCR-ABL-IN-7 可以用于慢性髓系白血病 (CML) 的研究。 | |||
T63746 |
Vamotinib
PF-114 |
Apoptosis; Tyrosine Kinases; Bcr-Abl | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Vamotinib (PF-114) 是一种具有口服活性和特异性的酪氨酸激酶抑制剂,具有抗增殖和抗肿瘤活性。Vamotinib 抑制 BCR/ABL 和 BCR/ABL-T315I 的磷酸化,促使细胞凋亡。Vamotinib 可用于研究耐药性费城染色体阳性 (Ph+) 白血病和阿尔茨海默症。 | |||
T64338 |
AKI603
AKI 603,AKI-603 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。 | |||
T3068 |
AT9283
J-504568 |
Apoptosis; FLT; JAK; Bcr-Abl; Aurora Kinase; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
AT9283 (J-504568) 是一种多靶点激酶抑制剂,抑制多种实体瘤在体内外的生长和存活,有效抑制Aurora A/B,JAK2/3,Abl (T315I),和Flt3,IC50值范围为 1-30 nM。 | |||
T60081 |
BV02
2-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1,3-dioxoisoindoline-5-carboxylic acid |
Others | Others |
BV02 是 14-3-3 蛋白-蛋白相互作用的抑制剂,可用于治疗慢性粒细胞白血病的研究。 BV02 破坏表达 IM 抗性 T315I 突变和 IM 敏感的野生型 Bcr-Abl 的造血细胞。 | |||
T2640 |
Rebastinib
DCC2036,DCC 2036,DCC-2036 |
Apoptosis; FLT; Bcr-Abl; Src | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Rebastinib (DCC-2036) 是一种口服有效的,非 ATP 竞争性的 Bcr-Abl 抑制剂,作用于 Abl1WT 和 Abl1T315I,IC50分别为 0.8 nM 和 4 nM,还抑制 LYN、SRC、HCK、FGR、FLT3、KDR 和 Tie-2,对 c-Kit 的活性低。Rebastinib 对 Angiopoietin2-Tie2通路具有抑制作用。 | |||
T6311 |
Bafetinib
NS-187,巴氟替尼,INNO-406 |
Bcr-Abl; Src; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Bafetinib (INNO-406) 是一种特异性双重 Bcr-Abl/Lyn 抑制剂,IC50值为5.8和19 nM。 | |||
T10489 |
BCR-ABL-IN-2
|
Others | Others |
BCR-ABL-IN-2 is a BCR-ABL1 tyrosine kinase inhibitor (IC50s: 57 nM, 773 nM for ABL1 native and ABL1 T315I). | |||
T27555 |
HS-438
HS 438 |
||
HS-438 inhibits imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia. | |||
T24872 |
TG101114
TG 101114,TG-101114 |
||
TG101114 is the T315I mutant enzyme inhibitor that acts by exhibiting reasonable in vivo efficacy in a xenograft mouse model harboring T315I. | |||
T15056 | DB07107 | Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
DB07107 is a potent inhibitor of drug resistant T315I mutant Bcr-Abl tyrosine kinase and a potent Akt1 inhibitor (IC50: 360 nM). | |||
T24496 |
MPT0B002
MPT-0-B-002,MPT 0 B 002 |
||
MPT0B002 is a microtubule inhibitor that acts by downregulating T315I mutant Bcr-Abl and inducing apoptosis of imatinib-resistant chronic myeloid leukemia cells. | |||
T69045 |
ON012380
|
||
ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I. | |||
T64087 | GZD856 formic | ||
GZD856 formic 是一种有效的和具有口服活性的PDGFRα/β抑制剂,IC50值分别为 68.6 和 136.6 nM。GZD856 formic 也是Bcr-AblT315I 的抑制剂,对天然Bcr-Abl 和 T315I 突变型的IC50值分别为 19.9 和 15.4 nM。GZD856 formic 具有抗肿瘤活性。 | |||
T63932 |
BCR-ABL-IN-4
|
||
BCR-ABL-IN-4 是 BCR-ABLL 抑制剂,表现出抗癌活性。BCR-ABL-IN-4 对癌细胞生长具有抑制作用,能够作用于 K562 细胞 (IC50: 0.67 nM) 和 BCR-ABL T315I 转染的 Ba/F3 细胞 (IC50: 16 nM)。 | |||
T38653 |
HG-7-85-01
|
||
HG-7-85-01 is a type II ATP competitive inhibitor targeting wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. It effectively inhibits T315I mutant Bcr-Abl kinase, as well as KDR and RET kinases with IC50 values of 3 nM, 20 nM, and 30 nM, respectively. In contrast, HG-7-85-01 exhibits weak or no inhibition towards other kinases (IC50 >2 μM). Furthermore, this compound inhibits cell proliferation through the induction of apoptosis and by impeding cell-cycle progres... | |||
T2802 |
Nocodazole
诺考达唑,R17934,Oncodazole |
Apoptosis; Microtubule Associated; Bcr-Abl; Autophagy; CRISPR/Cas9 | Angiogenesis; Apoptosis; Autophagy; Cytoskeletal Signaling; DNA Damage/DNA Repair; Tyrosine Kinase/Adaptors |
Nocodazole (Oncodazole) 是一种微管聚合抑制剂,具有可逆性,也是一种 Bcr-Abl 的抑制剂。Nocodazole 具有抗肿瘤活性,可以阻滞细胞周期,诱导细胞凋亡。 | |||
T68581 |
AP23464
|
||
AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the lo... | |||
T11523 |
GZD856
|
PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
GZD856 is an orally bioavailable PDGFRα/β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities. |