Ponatinib (AP24534)

For research use only. Not for use in humans.

製品コードS1490

Ponatinib (AP24534)化学構造

CAS No. 943319-70-8

Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 18600
JPY 20200
JPY 63400
JPY 163000
最寄りの販売代理店を探す

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください:[email protected]

バルク問合せ

文献中Selleckの製品使用例(150)

製品安全説明書

Bcr-Abl阻害剤の選択性比較

生物活性

製品説明 Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
ターゲット
Abl [1]
(Cell-free assay)
PDGFRα [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
c-Src [1]
(Cell-free assay)
0.37 nM 1.1 nM 1.5 nM 2.2 nM 5.4 nM
体外試験

AP24534 potently inhibits native Abl, AblT315I, and other clinically important Abl kinase domain mutants with IC50 of 0.30 nM–2 nM. AP24534 doesn't inhibit Aurora kinase family members, nor does it inhibit insulin receptor or CDK2/cyclin E. AP24534 inhibits proliferation of Ba/F3 cells expressing Bcr-Abl with IC50 of 0.5 nM, as well as Ba/F3 cells expressing a range of Bcr-Abl mutants with IC50 of 0.5 nM–36 nM. The inhibition of proliferation by AP24534 is correlated with induction of apoptosis. [1-2] In leukemic cell lines containing activated forms of FLT3, KIT, FGFR1, and PDGFRα receptors, AP24534 potently inhibits receptor phosphorylation and cellular proliferation with IC50 of 0.3 nM to 20 nM. In MV4-11 (FLT3-ITD(+/+)) but not RS4;11 (FLT3-ITD(–/–)) AML cells, AP24534 inhibits FLT3 signaling and induced apoptosis at less than 10 nM. AP24534 inhibits viability of primary leukemic blasts from a FLT3-ITD positive AML patient with IC50 of 4 nM but not those from patients with AML expressing native FLT3. [3] In Ba/F3 cells engineered to express activated FGFR1-4, AP24534 potently inhibits FGFR-mediated signaling and viability with IC50 lower than 40 nM. In cell lines representing multiple tumor types (endometrial, bladder, gastric, breast, lung, and colon), and containing FGFRs dysregulated by a variety of mechanisms, AP24534 inhibits FGFR-mediated signaling with IC50 less than 40 nM and inhibits cell growth with IC50 of 7 nM–181 nM. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell NH\5O2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHqTWM2OD1yLkCwNFAxODB|NUmg{txO MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
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MEG-01 NV;TRopST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXsTWM2OD1yLkCwNFEzQCEQvF2= NYD0W|E6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
LAMA-84 NYfOeIMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPxTWM2OD1yLkCwNFE3PSEQvF2= NXraTY5SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
CGTH-W-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TkO2lEPTB;MD6wNFE3QSEQvF2= M2jTXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
KASUMI-1 M{OxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTtNWNnUUN3ME2wMlAxOjF5IN88US=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
BE-13 MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDVcW5KSzVyPUCuNFAzPTlizszN MkTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
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NCI-H1623 NFSzV3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTR|LkS2OEDPxE1? NXnZOWM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
KNS-81-FD NUL6VGpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWi1fmxSUUN3ME20N{44PjJizszN NHzNS209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
TGBC1TKB MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjCfYlKSzVyPUSzMlkxQTlizszN M{Luc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
RERF-LC-MS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHt[Y44UUN3ME20N{46OjhzIN88US=> M1fZVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
PC-3 NFTIb5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jHUWlEPTB;NESuOFM1PyEQvF2= Mkf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
HuP-T4 M4jU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrHTWM2OD12ND60OFc1KM7:TR?= MkfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
NCI-H510A MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn5NopoUUN3ME20OE44ODhizszN NHjCeYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LB2518-MEL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO0TWM2OD12ND63PVM4KM7:TR?= NFHI[WY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
TE-5 NFnSXHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXWTWM2OD12NT65OVgyKM7:TR?= Ml6xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
EW-24 NE\LT4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzGN2ZKSzVyPUS2MlE4OjNizszN NF\hNng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LB647-SCLC NE\ES2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\kTWM2OD12Nj6yNVU2KM7:TR?= MmTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
NCI-H524 M1fn[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\KXW1bUUN3ME20Ok44OTh3IN88US=> NFrEOJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
EW-11 NG\W[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3n5eGlEPTB;NE[uPVM4OyEQvF2= NHLtV4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
KALS-1 MnLjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR5LkKwOlYh|ryP M2n1NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEyPzF6M{evK|5USU6JRWK8M4E,
BT-474 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\J[pN[UUN3ME20O{41OjF4IN88US=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
SK-N-AS MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH32PHVKSzVyPUS3Mlg5QCEQvF2= NWTOW5lwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
HCC2157 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXHWmhKSzVyPUS4MlA4PiEQvF2= NFfDVW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
HCC1954 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvLblZJUUN3ME20PE4yPzB2IN88US=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>
FADU NGD0eHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrVOYU4UUN3ME20PE4{ODNzIN88US=> NYPFWIplRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTF5MUizO{8oRlODTlfFVlww[T5?
S-117 NULQNGh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTtTmNKSzVyPUS4MlM5OTVizszN MnfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVE4OTh|Nz:nQnNCVkeHUkyvZV4>
LS-1034 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXmTXZMUUN3ME20PE44ODZ5IN88US=> NGizenM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
CAMA-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLrWoxKUUN3ME20PU42PTR|IN88US=> NH\yWWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
LU-134-A MkHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4S3[mlEPTB;NEmuPFA5PSEQvF2= NHL1c3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOTdzOEO3M{c,W0GQR1XSQE9iRg>?
NCI-H1838 NXzBW5hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTR7LkiwPFch|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNVcyQDN5Lze+V2FPT0WUPD;hQi=>

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アッセイ
Methods Test Index PMID
Western blot
pSrc / Src / pPlcg / Plcg / pStat5 / Stat5 ; 

PubMed: 22781593     


In (B) inhibition of Src, Plcg and Stat5 was seen in MLNAF cell lines treated with Ponatinib; ZNF112 expresses ZMYM2–FGFR1, CEP2A and CEP5A cells express CEP110–FGFR1 and BBC2 expresses BCR–FGFR1.

pFGFR1(pY20) / FGFR1; 

PubMed: 22781593     


Western blot analysis, using various antibodies specific for downstream targets of FGFR1, demonstrates that Ponatinib inhibits the activation of Plcg and Src as a result of inhibiting the FGFR1 fusion kinase in human KG1 cells. 

cleaved caspase-3 / cleaved caspase-7 / BAX / Bcl-2; 

PubMed: 30959969     


Western blot analysis of cleaved caspase-3, cleaved caspase-7, Bax, Bcl-2, and β-Tubulin (control) in treated cells.

p-Rb(S807/811) / Rb / CDK4 / CDK6 / Cyclin D1 / CDK2 / Cyclin E1; 

PubMed: 30959969     


Western blot analysis of Rb/p-Rb, CDK4, CDK6, Cyclin D1, CDK2, Cyclin E1, and β-Tubulin (control) in the SK-Hep-1 and SNU-423 cells treated with ponatinib. 

RAD51; 

PubMed: 30959969     


The effect of ponatinib on the concentration of Rad51 in SK-Hep-1 and SNU-423 cells.

p-MEK / MEK / p-ERK / ERK; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of Mek and Erk. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

c-Jun / p-JNK(T183/Y185) / JNK; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of JNK and c-Jun. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

p-p38 MAPK / p38 MAPK; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of p38. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

p-JAK2 / JAK2 / p-STAT3 / STAT3; 

PubMed: 30959969     


Effect of ponatinib on the phosphorylation of Jak2, and Stat3. Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was used as a control.

PI3K p85 / p-PI3K / p-PDK1 / PDK1 / p-mTOR / mTOR; 

PubMed: 30959969     


Effects of ponatinib on the protein concentration and phosphorylation of PI 3-kinase, PDK1, Akt, and mTOR in HCC cells. 

p-PDGFRα / PDGFRα; 

PubMed: 24472312     


Ponatinib inhibited phosphorylation of PDGFRα in a concentration-dependent manner. EOL-1 and BaF3-WT or -T674I FIP1L1-PDGFRα cells were exposed to escalating concentrations of ponatinib for 24 h.

PARP / Caspase-3 / Active Caspase-3; 

PubMed: 24472312     


The concentration- (for 24 h) and time-dependent (1 nM for EOL-1, 300 nM for BaF3-WT and -T674I FIP1L1-PDGFRα cells) cleavage of PARP and caspase-3 triggered by ponatinib was analyzed by immunoblotting.

AIF / Cyto C ; 

PubMed: 24472312     


Ponatinib elicited release of AIF and cytochrome c into the cytosol. Cells were treated with 1 nM ponatinib for the indicated durations and the cytosolic fraction was extracted with digitonin buffer. Levels of AIF and Cytochrome c (Cyto c) were detected by immunoblotting.

Mcl-1 / Survivin / Bcl-Xl / XIAP / Bax / Bcl-2 / Bim; 

PubMed: 24472312     


Immunoblotting of apoptosis-related proteins in CEL cells after treatment for 24 h.

β-catenin ; 

PubMed: 24472312     


Ponatinib concentration-dependently lowered β-catenin. EOL-1 cells were incubated with ponatinib for 24 h, and cytoplasmic and nuclear extracts were determined by immunoblotting.

β-catenin; 

PubMed: 24472312     


Analysis of β-catenin localization. EOL-1 cells were pretreated with 1 nM ponatinib for 24 h, immunofluorescence analysis was performed with anti-β-catenin. Nuclei were stained with 4,6-diamidino-2-phenylindole (DAPI). 

ABL; 

PubMed: 19878872     


In vitro [γ-32P]-ATP autophosphorylation of full-length (A) ABL or (B) ABLT315I kinase treated with AP24534, imatinib, nilotinib, or dasatinib. After incubation of tyrosine-dephosphorylated enzyme with the indicated inhibitor in the presence of [γ-32P]-ATP and separation by SDS-PAGE, signal intensity was measured by autoradiography.

22781593 30959969 24472312 19878872
Growth inhibition assay
Cell viability; 

PubMed: 30174789     


(A) Effect of Ponatinib on basal viability of HUVECs. The cells were treated with Ponatinib at indicated concentrations or 0.1% DMSO (vehicle control) for 24 h.

30174789
体内試験 In a mouse xenograft model of Ba/F3 cells expressing native Bcr-Abl, AP24534 (2.5 mg/kg and 5 mg/kg) prolongs mice median survival. In the xenograft model of Ba/F3 Bcr-AblT315I, AP24534 (10 mg/kg–50 mg/kg) significantly suppresses tumor growth. AP24534 (30 mg/kg) decreases the phosphorylated Bcr-Abl and phosphorylated CrkL levels in the tumors. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

Peptide substrate phosphorylation assays with GST-Abl kinase domains:

The effect of AP24534 (0-320 nM) on GST-Abl kinase activity is assessed by using a synthetic peptide substrate (Abltide: EAIYAAPFAKKK). Assays are carried out at 30 °C for 15 min in 25 μL reaction mixture: 8 mM MOPS (pH 7), 0.2 mM EDTA, 50 μM Abltide, 30 mM MgCl2, 10 mM β-glycerol phosphate, 1 mM EGTA, 0.002% Brij-35, 0.4 mM DTT, 0.2 mg/mL BSA, 0.4 mM sodium orthovanadate, 10 nM WT or mutant GST-Abl kinase, and 100 µM ATP/γ-32[P]ATP (5000 cpm/pmol). Reactions are terminated by transferring a portion of the reaction mixture onto a p81 phosphocellulose filter and immersing in 0.75% phosphoric acid. Filters are washed 3 times in 0.75% phosphoric acid, rinsed in acetone, and air dried; phosphate incorporation is determined by scintillation counting. All results are corrected for background binding to the filters, as determined by omitting peptide substrate from the kinase reaction. Time course experiments to establish the linear range of enzymatic activity precedes kinase assays.
細胞試験: [2]
- 合併
  • 細胞株: Ba/F3 cells expressing Bcr-Abl or a range of single mutations in the kinase domain of Bcr-Abl
  • 濃度: 0-625 nM
  • 反応時間: 72 hours
  • 実験の流れ: Ba/F3 cell lines are distributed in 96-well plates (4 × 103 cells/well) and incubated with AP24534 for 72 hours. Proliferation is measured using a methanethiosulfonate (MTS)-based viability assay (CellTiter96 Aqueous One Solution). All values are normalized to the control wells with no drug. IC50 values are reported as the mean of three independent experiments performed in quadruplicat
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: Mouse xenograft models of Ba/F3 cells expressing Bcr-Abl or Bcr-AblT315I
  • 投薬量: 2.5 mg/kg and 5 mg/kg for Ba/F3 Bcr-Abl; 2.5 mg/kg–50 mg/kg for Ba/F3 Bcr-AblT315I
  • 投与方法: Oral gavage once daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 30 mg/mL (56.33 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
1% CMC Na
混合させたのち直ちに使用することを推奨します。
30mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 532.56
化学式

C29H27F3N6O

CAS No. 943319-70-8
Storage powder
in solvent
別名 N/A
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CN=C5N4N=CC=C5

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04554459 Recruiting Drug: Ponatinib 15 MG Oral Tablet Acute Lymphoblastic Leukemia Adult|Ph+ ALL|Newly Diagnosed Institute of Hematology and Blood Transfusion Czech Republic|CZECRIN - Czech Clinical Research Infrastructure Network February 16 2021 Phase 2
NCT04160546 Recruiting Drug: Ponatinib 15 MG|Drug: Acetylsalicylic acid 100 MG Chronic Myeloid Leukemia Chronic Phase Fundacion CRIS de Investigación para Vencer el Cáncer|Incyte Biosciences UK|Apices Soluciones S.L. January 17 2020 Phase 2
NCT03934372 Recruiting Drug: Ponatinib Acute Myeloid Leukemia|Accelerated Phase Chronic Myeloid Leukemia|Blast Phase Chronic Myeloid Leukemia|Chronic Phase Chronic Myeloid Leukemia|Acute Lymphoblastic Leukemia|Acute Lymphocytic Leukemia|Leukemia|Lymphoma|Solid Tumors Incyte Biosciences International Sàrl|Incyte Corporation January 29 2020 Phase 1|Phase 2
NCT03690115 Recruiting Drug: Ponatinib 30 MG Leukemia Myeloid Acute Versailles Hospital December 2 2019 Phase 2

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問(FAQ)

  • 質問1:

    Is the pre-solubilized inhibitor suitable for in vivo whole animal studies? Whether the solvent contains any non-DMSO stabilizer?

  • 回答:

    Our 10mM Ponatinib in DMSO solution is in pure DMSO and there is not other stabilizer added. You can use it for animal study. The vehicle we suggest for Ponatinib is: 30% PEG400/0.5% Tween80/5% Propylene glycol. It is a milky suspension used for oral gavage.

Bcr-Ablシグナル伝達経路

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