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KW-2449 {[allProObj[0].p_purity_real_show]}

货号:A306611

KW-2449 是一种多靶点激酶抑制剂,对FLT3ABLABLT315I和Aurora激酶的IC50值分别为6.6 nM、14 nM、4 nM和48 nM。

KW-2449 化学结构 CAS号:1000669-72-6
KW-2449 化学结构
CAS号:1000669-72-6
KW-2449 3D分子结构
CAS号:1000669-72-6
KW-2449 化学结构 CAS号:1000669-72-6
KW-2449 3D分子结构 CAS号:1000669-72-6
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KW-2449 纯度/质量文件 产品仅供科研

货号:A306611 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

99%+
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

98%
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

99%
LDN-214117 ++

ALK2, IC50: 24 nM

98%
DMH-1 +

ALK2, IC50: 107.9 nM

99%+
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

99%+
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

99%+
Alantolactone 98%
SIS3 97%
Pirfenidone 98%
Hesperetin 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

98%
GW788388 +++

ALK5, IC50: 18 nM

98%
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

98%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

99%+
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

99%+
Galunisertib ++

TβRI, IC50: 56 nM

98%
SB 431542 +

ALK5, IC50: 94 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Aurora A Aurora B Aurora C 其他靶点 纯度
BI-847325 ++

Aurora A (Human), IC50: 25 nM

++++

Aurora B (Xenopus laevis), IC50: 3 nM

++

Aurora C (Human), IC50: 15 nM

99%+
CCT 137690 ++

Aurora A, IC50: 15 nM

++

Aurora B, IC50: 25 nM

++

Aurora C, IC50: 19 nM

99%+
MK-5108 ++++

Aurora A, IC50: 0.064 nM

99%+
KW-2449 +

Aurora A, IC50: 48 nM

FLT3 99%+
Tozasertib ++++

Aurora A, Ki app: 0.6 nM

++

Aurora B, Ki app: 18 nM

+++

Aurora C, Ki app: 4.6 nM

Bcr-Abl,FLT3 99%+
AT9283 ++++

Aurora A, IC50: ~3.0 nM

++++

Aurora B, IC50: ~3.0 nM

99%+
MLN8054 +++

Aurora A, IC50: 4 nM

+

Aurora B, IC50: 172 nM

99%+
ZM-447439 +

Aurora A, IC50: 110 nM

+

Aurora B, IC50: 130 nM

Src 99%+
TCS7010 ++++

Aurora A, IC50: 3.4 nM

99%+
TAK-901 ++

Aurora A-TPX2, IC50: 21 nM

++

Aurora B-INCENP, IC50: 15 nM

99%+
Danusertib +++

Aurora A, IC50: 13 nM

+

Aurora B, IC50: 79 nM

+

Aurora C, IC50: 61 nM

RET 99%+
MK-8745 ++++

Aurora A, IC50: 0.6 nM

99+%
PHA-680632 ++

Aurora A, IC50: 27 nM

+

Aurora B, IC50: 135 nM

+

Aurora C, IC50: 120 nM

FLT3 99%+
AMG 900 +++

Aurora A, IC50: 5 nM

+++

Aurora B, IC50: 4 nM

++++

Aurora C, IC50: 1 nM

99%+
Alisertib ++++

Aurora A, IC50: 1.2 nM

99%+
ENMD-2076 +++

Aurora A, IC50: 14 nM

+

Aurora B, IC50: 350 nM

RET,FLT3 98%
JNJ-7706621 +++

Aurora A, IC50: 11 nM

++

Aurora B, IC50: 15 nM

99%+
CYC-116 +++

Aurora A, Ki: 8 nM

+++

Aurora B, Ki: 9 nM

FLT3 99%+
Reversine +++

Aurora A, IC50: 12 nM

+++

Aurora B, IC50: 13 nM

++

Aurora C, IC50: 20 nM

98%
CCT129202 ++

Aurora A, IC50: 42 nM

+

Aurora B, IC50: 198 nM

+

Aurora C, IC50: 227 nM

98%
SNS-314 mesylate +++

Aurora A, IC50: 9 nM

++

Aurora B, IC50: 31 nM

++++

Aurora C, IC50: 3 nM

99%+
Barasertib-HQPA ++++

Aurora B, IC50: 0.37 nM

99%+
Hesperadin +

Aurora B (human), IC50: 250 nM

98%
GSK-1070916 ++++

Aurora B-INCENP, IC50: 3.5 nM

+++

Aurora C-INCENP, IC50: 6.5 nM

Tie-2,SIK 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 FLT3 其他靶点 纯度
R406 Syk 98%
Go6976 99%+
Quizartinib +++

FLT3 (ITD), IC50: 1.1 nM

FLT3 (WT), IC50: 4.2 nM

98%
Gilteritinib ++++

FLT3, IC50: 0.29 nM

99%+
Amuvatinib +

FLT3 (D835Y), IC50: 81 nM

99%+
Pacritinib ++

FLT3, IC50: 22 nM

FLT3 (D835Y), IC50: 6 nM

97%
Dovitinib ++++

FLT3, IC50: 1 nM

c-Kit 99%+
Denfivontinib ++++

FLT3, IC50: 0.4 nM

FLT3 (D835Y), IC50: 0.4 nM

RET 99%+
TAK-659 HCl ++

FLT3, IC50: 4.6 nM

Syk 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 FGFR FGFR1 FGFR2 FGFR3 FGFR4 其他靶点 纯度
Tyrphostin AG1296 +

FGFR (Swiss 3T3), IC50: 12.3 μM

PDGFR 99%+
Pazopanib +

FGFR, IC50: 140 nM

99%
Erdafitinib RET 99%+
Gambogenic acid 98+%
Sulfatinib +++

FGFR1, IC50: 15 nM

99+%
Nintedanib esylate +

FGFR1, IC50: 69 nM

++

FGFR2, IC50: 37 nM

+

FGFR3, IC50: 108 nM

98%
Zoligratinib +++

FGFR1, IC50: 9.3 nM

+++

FGFR2, IC50: 7.6 nM

++

FGFR3, IC50: 22 nM

+

FGFR4, IC50: 290 nM

99%+
MK-2461 +

FGFR1, IC50: 65 nM

++

FGFR2, IC50: 39 nM

++

FGFR3, IC50: 50 nM

98%+
SU 5402 ++

FGFR1, IC50: 30 nM

98%
Brivanib +

FGFR1, IC50: 148 nM

99%+
Lucitanib ++

FGFR1, IC50: 17.5 nM

+

FGFR2, IC50: 82.5 nM

99%+
Ponatinib ++++

FGFR1, IC50: 2.2 nM

98%
PD-166866 +

FGFR1, IC50: 52.4 nM

98%
Narazaciclib ++

FGFR1, IC50: 26 nM

RET 99%+
Lactate +++

FGFR1, IC50: 8 nM

+++

FGFR3, IC50: 9 nM

c-Kit,FLT3 85%
Lenvatinib mesylate ++

FGFR1, IC50: 46 nM

c-RET 99%
LY2874455 ++++

FGFR1, IC50: 2.8 nM

++++

FGFR2, IC50: 2.6 nM

+++

FGFR3, IC50: 6.4 nM

+++

FGFR4, IC50: 6 nM

99%+
FIIN-2 +++

FGFR1, IC50: 3.09 nM

+++

FGFR2, IC50: 4.3 nM

++

FGFR3, IC50: 27 nM

++

FGFR4, IC50: 45.3 nM

98%
FIIN-3 +++

FGFR1, IC50: 13.1 nM

++

FGFR2, IC50: 21 nM

++

FGFR3, IC50: 31.4 nM

++

FGFR4, IC50: 35.3 nM

98%
Infigratinib ++++

FGFR1, IC50: 0.9 nM

++++

FGFR2, IC50: 1.4 nM

++++

FGFR3, IC50: 1.0 nM

FGFR3 (K650E), IC50: 4.9 nM

+

FGFR4, IC50: 60 nM

99%+
Danusertib ++

FGFR1, IC50: 47 nM

RET 99%+
R1530 ++

FGFR1, IC50: 28 nM

98%
ENMD-2076 +

FGFR1, IC50: 92.7 nM

+

FGFR2, IC50: 70.8 nM

RET,FLT3 98%
Dovitinib +++

FGFR1, IC50: 8 nM

+++

FGFR3, IC50: 9 nM

c-Kit,FLT3 99%+
Sorafenib +

FGFR1, IC50: 580 nM

99%
SSR128129E +

FGFR1, IC50: 1.9 μM

99%+
AZD-4547 ++++

FGFR1, IC50: 0.2 nM

++++

FGFR2, IC50: 2.5 nM

++++

FGFR3, IC50: 1.8 nM

98%
Lenvatinib ++

FGFR1, IC50: 46 nM

RET 98%
PD173074 ++

FGFR1, IC50: ~25 nM

99%+
S49076 ++

FGFR1, IC50: 18 nM

+++

FGFR2, IC50: 17 nM

+++

FGFR3, IC50: 15 nM

98%
Futibatinib ++++

FGFR1, IC50: 1.8 nM

++++

FGFR2, IC50: 1.4 nM

++++

FGFR3, IC50: 1.6 nM

+++

FGFR4, IC50: 3.7 nM

99%+
Ferulic Acid +

FGFR1, IC50: 3.78 μM

+

FGFR2, IC50: 12.5 μM

98%
Nintedanib +

FGFR1, IC50: 69 nM

++

FGFR2, IC50: 37 nM

+

FGFR3, IC50: 108 nM

+

FGFR4, IC50: 610 nM

99+%
ASP5878 ++++

FGFR1, IC50: 0.47 nM

++++

FGFR2, IC50: 0.6 nM

++++

FGFR3, IC50: 0.74 nM

+++

FGFR4, IC50: 3.5 nM

98%
PRN1371 ++++

FGFR1, IC50: 0.6 nM

++++

FGFR2, IC50: 1.3 nM

+++

FGFR3, IC50: 4.1 nM

++

FGFR4, IC50: 19.3 nM

99%
Derazantinib +++

FGFR1, IC50: 4.5 nM

++++

FGFR2, IC50: 1.8 nM

+++

FGFR3, IC50: 4.5 nM

++

FGFR4, IC50: 34 nM

RET 99%+
ODM-203 +++

FGFR1, IC50: 11 nM

+++

FGFR2, IC50: 16 nM

+++

FGFR3, IC50: 6 nM

++

FGFR4, IC50: 35 nM

99%+
Pemigatinib ++++

FGFR1, IC50: 0.4 nM

++++

FGFR2, IC50: 0.5 nM

++++

FGFR3, IC50: 1.2 nM

++

FGFR4, IC50: 30 nM

99%+
SKLB 610 PDGFR 99%+
Alofanib 99%+
Lirafugratinib 98%
Masitinib mesylate FAK 99%+
BLU9931 +

FGFR3, IC50: 150 nM

+++

FGFR4, IC50: 3 nM

99%+
BO-264 99%+
Fisogatinib +++

FGFR4, IC50: 5 nM

99%+
H3B-6527 ++++

FGFR4, IC50: <1.2 nM

99%+
Roblitinib ++++

FGFR4, IC50: 1.9 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Abl Bcr-Abl 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

99%+
KW-2449 +++

Abl (T315I), IC50: 4 nM

Abl, IC50: 14 nM

FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

Tie-2,FLT3 99%+
PP121 ++

Abl, IC50: 18 nM

PDGFR,VEGFR 99%+
GNF-7 +++

E255V, IC50: 122 nM

M351T, IC50: 133 nM

99%+
Olverembatinib dimesylate ++++

Abl (G250E), IC50: 0.35 nM

Abl, IC50: 0.34 nM

99%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

98+%
GNF-2 +

Bcr-Abl (K562 cell line), IC50: 273 nM

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

DUB 98+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

98%
Radotinib ++

BCR-ABL1, IC50: 34 nM

98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

KW-2449 生物活性

靶点
  • Aurora A

    Aurora A, IC50:48 nM

  • Abl

    Abl (T315I), IC50:4 nM

    Abl, IC50:14 nM

描述 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A, and showing little effect on PDGFRβ, IGF-1R, EGFR.

KW-2449 参考文献

[1]Shiotsu Y, Kiyoi H, et al. KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17.

[2]Pratz KW, Cortes J, et al. A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response. Blood. 2009 Apr 23;113(17):3938-46.

KW-2449 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.04mL

3.01mL

1.50mL

30.08mL

6.02mL

3.01mL

KW-2449 技术信息

CAS号1000669-72-6
分子式C20H20N4O
分子量 332.399
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(150.42 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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