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18

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1938	FLT3-IN-2	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	FLT3-IN-2 是 FLT3 抑制剂(IC50＜1 μM)。
T9856	FLT3-IN-10 2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	FLT3-IN-10 (2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-) (compound 7c) 是有效的 FMS 样酪氨酸激酶 3 (FLT3) 抑制剂。FLT3-IN-10 具有治疗 FLT3 突变的急性髓性白血病 (AML) 的潜力。
T11707	JAK2/FLT3-IN-1	JNK	MAPK
	JAK2/FLT3-IN-1 has anti-cancer activity. JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively.
T63274	FLT3/ITD-IN-2
	FLT3/ITD-IN-2 是 FLT3-ITD 的有效抑制剂，能够作用于 FLT3D835Y (IC50: 0.3 nM)、FLT3(IC50: 0.4 nM)和 FLT3-ITD(IC50: 1.0 nM)。FLT3/ITD-IN-2 能够有效的抑制 FLT3 的磷酸化，能够有效的抑制急性髓系白血病细胞的增殖。
T63629	PDGFRα/FLT3-ITD-IN-2
	PDGFRα/FLT3-ITD-IN-2 是 PDGFRα (IC50>20 μM) 和 FLT3 (IC50: 0.004 μM) 的有效抑制剂。PDGFRα/FLT3-ITD-IN-2 对急性髓系白血病或慢性嗜酸性粒细胞白血病表现出研究潜力。
T9017	HPK1-IN-2 Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2,HPK1-IN-2	Others; FLT; Src	Angiogenesis; Others; Tyrosine Kinase/Adaptors
	HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) 是一种有效且具有口服活性的造血祖细胞激酶-1 抑制剂(HPK1；IC50<0.05 µM)。它还抑制 Lck (0.05 µM<IC50<0.5 µM) 和 Flt3 (IC50<0.05 µM) 激酶活性，具有抗肿瘤活性。
T3211	Midostaurin 米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱	Others; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Others
	Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂，有抗肿瘤活性，对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。
T35900	JAK2-IN-7 JAK2-IN-7	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JAK2-IN-7 是一种选择性 JAK2抑制剂，对 JAK2，SET-2 和 Ba/F3V617F 细胞的IC50为 3、11.7 和 41 nM。 JAK2-IN-7 的选择性是 JAK1, JAK3，FLT3 的 14 倍以上。JAK2-IN-7 刺激细胞周期停滞在 G0/G1 期，并诱导肿瘤细胞凋亡 (apoptosis)，具有抗肿瘤活性。
T2054	Altiratinib DCC-2701	VEGFR; Tie-2; FLT; Trk receptor; c-Met/HGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Altiratinib (DCC-2701) 是一种多靶点激酶抑制剂，能够抑制 MET (IC50:2.7 nM)，TIE2 (IC50:8 nM)，VEGFR2 (IC50:9.2 nM)，FLT3 (IC50:9.3 nM)，Trk1 (IC50:0.85 nM)，Trk2 (IC50:4.6 nM) 和 Trk3 (IC50:0.83 nM)。
T81421	Pomalidomide-C5-Dovitinib	PROTACs	PROTAC
	Pomalidomide-C5-Dovitinib（compound 2）是链接Pomalidomide与Dovitinib的PROTAC，且与CRBN结合。该化合物在FLT3-ITD+ AML细胞中表现出增强的抗增殖能力，通过泛素-蛋白酶体依赖性途径促进FLT3-ITD和KIT蛋白的降解，并彻底抑制其下游信号传导，显示出研究FLT3-ITD+急性髓系白血病的潜力。
T60760	HDAC10-IN-2
	HDAC10-IN-2 (化合物 10c) 调节侵袭性 FLT3-ITD 阳性急性髓系白血病细胞的自噬。HDAC10-IN-2是HDAC10的高选择性抑制剂 (IC50 = 20 nM)。
T78145	HDAC10-IN-2 hydrochloride	Autophagy	Autophagy
	HDAC10-IN-2 hydrochloride（化合物10c）是一种对HDAC10具有高效性和高选择性的抑制剂，IC50值为20 nM。该化合物能够调控FLT3-ITD阳性急性髓系白血病细胞的自噬过程。
T37085	Luxeptinib
	Luxeptinib (CG-806) is a novel pan-FLT3/pan-BTK inhibitor that is administered orally. It exhibits potent and reversible inhibition of these enzymes, acting through a non-covalent mechanism. Luxeptinib effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells [1][2][3][4].
T61755	E6201
	E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2].
T29062	UNC3133 UNC 3133,UNC-3133
	UNC3133 is a potent and selective Mer tyrosine kinase (MerTK) inhibitor with IC50 Mer 3.0 nM; Axl 17nM; Tyro 3.31 nM; FLT3 6.6 nM; PO Cmax = 0.023; IV T1/2 = 1.59 h, %F = 16. Mer tyrosine kinase (MerTK) is aberrantly elevated in various tumor cells and ha
T62417	MELK-8a
	MELK-8a (NVS-MELK8a) 是一种高效的、选择性的母体胚胎亮氨酸拉链激酶 (MELK) 抑制剂 (IC50: 2 nM)。MELK-8a 也能够抑制 Flt3 (ITD) (IC50: 0.18 μM)、Haspin (IC50: 0.19 μM)、PDGFRα (IC50: 0.42 μM)。其中 MELK 在调节癌细胞的细胞有丝分裂中具有重要作用。
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...
T71382	KRC-108
	KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumo...

化合物

Cat.No: T1938

Target: FLT

Cat.No: T9856

Synonym: 2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-

Target: FLT

JAK2/FLT3-IN-1

Cat.No: T11707

Target: JNK

FLT3/ITD-IN-2

Cat.No: T63274

PDGFRα/FLT3-ITD-IN-2

Cat.No: T63629

Cat.No: T9017

Synonym: Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2,HPK1-IN-2

Target: Others, FLT, Src

Cat.No: T3211

Synonym: 米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱

Target: Others, PKC

Cat.No: T35900

Synonym: JAK2-IN-7

Target: JAK

Cat.No: T2054

Synonym: DCC-2701

Target: VEGFR, Tie-2, FLT, Trk receptor, c-Met/HGFR

Pomalidomide-C5-Dovitinib

Cat.No: T81421

Target: PROTACs

Cat.No: T60760

HDAC10-IN-2 hydrochloride

Cat.No: T78145

Target: Autophagy

Cat.No: T37085

Cat.No: T61755

Cat.No: T29062

Synonym: UNC 3133,UNC-3133

Cat.No: T62417

Cat.No: T68389

Cat.No: T71382

Cat. No.	Product Name	Target	Signaling Pathways
T6S0033	Crotonoside 巴豆苷；异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE	Others; FLT; HDAC	Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors
	Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。它抑制 FLT3 和 HDAC3/6，有治疗急性髓性白血病 (AML)的研究潜力。

天然产物

Cat.No: T6S0033

Synonym: 巴豆苷；异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE

Target: Others, FLT, HDAC

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