Obatoclax Mesylate (GX15-070)

Catalog No.S1057

For research use only.

Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.

Obatoclax Mesylate (GX15-070) Chemical Structure

CAS No. 803712-79-0

Selleck's Obatoclax Mesylate (GX15-070) has been cited by 107 publications

Purity & Quality Control

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Biological Activity

Description Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.
Features Potential 1st-in-class small molecule antagonist of Bcl-2 designed to inhibit all relevant Bcl-2 family members, including Mcl-1.
Targets
Bcl-2 [1]
(Cell-free assay)
0.22 μM(Ki)
In vitro

Obatoclax completely inhibits Bak recovery of Mcl-1 at 5 μM in SK-Mel5 cells and overcomes resistance to ABT-373-induced apoptosis conferred by Mcl-1 in KB/Bcl-2 cells. [1] Obatoclax is a BH3 mimetic which binds to a broad spectrum of Bcl-2 family members, including Bcl-2, Bcl-xL, and Mcl-1. Obatoclax uniquely displaces BH3 domains by activation of the pocket of Mcl-1 followed by a triggering of apoptosis mediated by oligomerization of Bak and release of cytochrome c. Obatoclax is sensitive to Bcl-xL in cell lines lacking it or showing low expression. It shows low cytotoxicity to Mcl-1, Bcl-2, and Bcl-xL in all the strongly-expressed cell lines. Obatoclax inhibits multiple myeloma (MM) cell lines (KMS12PE, KMS18, MY5, etc.) with IC50 values ranging from 52 to 1100 nM and the inhibition is umimpaired even in the presence of IL-6 or IGF-1, which are resistance to cytotoxic agents, at a concentration of 150 nM. Obatoclax enhances the antimyeloma activity induced by melphalan, dexamethasone, or bortezomib. [2] Obatoclax potentiates TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-mediated apoptosis by unsequestering Bak and Bim from Bcl-2/Bcl-xL or Mcl-1 proteins in PANC-1 and BxPC-3 cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KARPAS-45 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ntSGlEPTB;MD6wNFAxOzF5IN88US=> NXPHfmJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
SK-MEL-30 NEDxNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMECwN|U2KM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
NALM-6 NUPWTW9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XIVWlEPTB;MD6wNFA{PTZizszN MmjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
KYSE-450 M2qxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HqW2lEPTB;MD6wNFA1PjlizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
BHY MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUiycVdJUUN3ME2wMlAxODZyMTFOwG0> NEL6NZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
GR-ST Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHqOpRWUUN3ME2wMlAxODZ2ODFOwG0> NF7NcHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
786-0 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\j[GFuUUN3ME2wMlAxODd5NjFOwG0> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
C-33-A M4\4b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjpTXJnUUN3ME2wMlAxODh2ODFOwG0> M2rNelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
BHT-101 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXtcHNXUUN3ME2wMlAxOTB4IN88US=> NWOz[4RURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
EB2 M1SwTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwMECxNVgh|ryP MlvsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
G-361 NHLVU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3MWYRKSzVyPUCuNFAyOjRizszN MnXkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
KE-37 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjFTWM2OD1yLkCwNVI5KM7:TR?= NVfC[ZRjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
MHH-PREB-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;1Z5RKSzVyPUCuNFAyPCEQvF2= NFzQfJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
MCF7 NY\0XGs4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7NS2JKSzVyPUCuNFAyPTlizszN NIHzdmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
LOUCY MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTZRVNKSzVyPUCuNFAyPzVizszN NFTiVWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
EW-7 Mnv2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXC[GZyUUN3ME2wMlAxOTd3IN88US=> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
KYSE-510 M13r[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S1cmlEPTB;MD6wNFI{OyEQvF2= NIXvTGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
SK-MEL-3 NELPc5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTBwMECyOlQh|ryP NUXkUWJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
HAL-01 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnrTWM2OD1yLkCwNlk4KM7:TR?= M{joc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
HCC2998 NXTzS3VZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTSWJVwUUN3ME2wMlAxOzN3IN88US=> Ml7lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
A375 NVHyd3JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PBN2lEPTB;MD6wNFM2KM7:TR?= M3nyblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
MZ7-mel MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMECzPVkh|ryP MlryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
SH-4 NVi0UGdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwMEC0NVch|ryP Mn;5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
HT-144 M3zoSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTBwMEC0N{DPxE1? M3vtUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
KYSE-140 NWnTelIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXnbZBKSzVyPUCuNFA1OzVizszN Mo\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
PSN1 M1fMUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXUe5pqUUN3ME2wMlAxPDZ5IN88US=> NGH1XZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
COLO-679 NGHHZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\FfmNKSzVyPUCuNFA1QThizszN NIjPZXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
SW620 M{nJcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvUTWM2OD1yLkCwOVEyKM7:TR?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
HGC-27 NYrXfo96T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjXT2JOUUN3ME2wMlAxPTJ2IN88US=> MorpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
IGROV-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\OdFFKSzVyPUCuNFA3KM7:TR?= M4j6[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
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IST-MEL1 NFrqS|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwMEC4NVgh|ryP M2PERlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
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NCI-H524 NVS5NZk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnuc4pxUUN3ME25MlU5PjJ6IN88US=> MnXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
KOSC-2 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr1TWM2OD17Lk[yPFM1KM7:TR?= NXe1NmQ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
T-24 NFrpUFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnsTWM2OD17Lkm0OFE2KM7:TR?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
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NCI-H23 NXfBSFVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFyLk[0OFIh|ryP MnXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
UACC-812 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXs[mY6UUN3ME2xNU44OTdizszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
SCLC-21H MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF{LkG1OVEh|ryP MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
NCI-SNU-16 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vxPGlEPTB;MUOuNVI2QCEQvF2= NVnqVlhURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
HD-MY-Z MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrv[Ig5UUN3ME2xOE43OzZ|IN88US=> M37iVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
SK-N-FI MmnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HaNGlEPTB;MUSuPFkyOiEQvF2= NIjWXpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
LB647-SCLC NF3VNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIKzOWZKSzVyPUG1MlcyQTVizszN Mn\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
NCI-H345 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf1SnhKSzVyPUG3MlM1OyEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
NCI-H1563 M{ezfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:4dYtKSzVyPUG4Mlc3ODFizszN MmP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
RL M3i1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTJzLkK2OVYh|ryP NXz2fI5oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
KY821 NYLQSGM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfoTWM2OD1{Mj6wOVU{KM7:TR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA4OzV6Lze+V2FPT0WUPD;hQi=>
JVM-3 NUDBfnVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXTO|l{UUN3ME2yOU4xPDF|IN88US=> M3G1WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
NCI-H1793 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVf0Rm1IUUN3ME2yPE42PDl7IN88US=> M1rSNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
LU-134-A MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLMVnZKSzVyPUOwMlIxOzdizszN NHO4[Xk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB5M{W4M{c,W0GQR1XSQE9iRg>?
NCI-H1395 NHjyR3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr5TWM2OD1|Mj6yOFMyKM7:TR?= M2SxW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODd|NUivK|5USU6JRWK8M4E,
NCI-H1993 NWPGemduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vUR2lEPTB;M{KuPFIyQCEQvF2= NWHnd2tNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
P31-FUJ MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTN|LkS4PVkh|ryP MnHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
LS-513 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;o[mlEPTB;M{WuPFg4QSEQvF2= MnvRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
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SW684 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLFSXJKSzVyPUSzMlk3PjFizszN NVLrV3M6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
COR-L88 M1fKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTXUGtpUUN3ME20OE4xPjZ3IN88US=> MkPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
NCI-H889 NED1dHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHBUI9KSzVyPUS1MlAxQDdizszN NUG0clIzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{O1PE8oRlODTlfFVlww[T5?
TALL-1 MmPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nn[GlEPTB;NE[uNVE6QSEQvF2= MmHuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
KARPAS-299 M3jJcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrJZWYxUUN3ME20O{4yQTl|IN88US=> MkDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzN3OD:nQnNCVkeHUkyvZV4>
Assay
Methods Test Index PMID
Western blot Cyclin D1 / p27 Kip1 ; p-Cyclin D1 ; p-GSK3β / GSK3β / p-ERK / ERK / p-p38 / p38 28382170 28035994
Growth inhibition assay Cell proliferation ; Cell viability 28035994 21368880
In vivo Obatoclax also exhibits high antitumor activity in SCID mice bearing human C33A cerivical carcinoma tumors at a dose of 0.5 mg/kg. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Bcl-2 Binding affinity calculation:

    A predicted binding affinity for Obatoclax binding to BCL-2 is calculated using the SIE scoring function. [4] As a control in determining the reliability of the calculation, predicted binding affinities Ki) are calculated for a set of 12 small molecules with experimentally measured binding affinities to BCL-2.

Cell Research:[2]
  • Cell lines: Human MM cells (HMCLs), peripheral blood lymphocytes (PBLs), bone marrow stromal cells (BMSCs)
  • Concentrations: ~10 μM
  • Incubation Time: 48-72 hours
  • Method: Obatoclax is dissolved in DMSO at a stock concentration of 5 mM. Cell viability is assayed by MTT. Human MM cells (HMCLs), peripheral blood lymphocytes (PBLs), bone marrow stromal cells (BMSCs) are seeded in 96-well plates at a density of 2 × 104 per well for HMCLs or 5~10 × 103 for PBLs. Various concentrations of Obatoclax are added to the cells, with or without IGF-1 (50 ng/mL) or IL-6 (10 ng/mL). Cells are incubated for 48-72 hours and cell viability is determined.
Animal Research:[1]
  • Animal Models: Female BALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells are used.
  • Dosages: 0.0313, 0.25, 0.5 and 2 mg/kg
  • Administration: Administered intravenously (tail vein) once a day

Solubility (25°C)

In vitro

DMSO 83 mg/mL
(200.73 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 413.49
Formula

C20H19N3O.CH4O3S

CAS No. 803712-79-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(N1)C=C2C(=CC(=C3C=C4C=CC=CC4=N3)N2)OC)C.CS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00438178 Completed Drug: Obatoclax mesylate (GX15-070MS) Hematological Malignancies Gemin X|Teva Branded Pharmaceutical Products R&D Inc. October 2005 Phase 1
NCT00600964 Completed Drug: GX15-070MS Chronic Lymphocytic Leukemia Gemin X|Teva Branded Pharmaceutical Products R&D Inc. September 2004 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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