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Fig. 1 · Structure
Cat. No.
A10665
CAS No.
803712-79-0
Formula
C20H19N3O.CH4O3S
Mol. Weight
413.5

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Obatoclax mesylate (GX15-070)

Bcl-2 Inhibitor

Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).

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Publications for Obatoclax mesylate

4 publications citing this product

  1. Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
  2. Silva S, .et al. , Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
  3. Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
  4. P Geserick, .et al. , Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
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For laboratory research use only. We do not sell to patients.

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Biological Activity

Target & Activity

Target Activity Value
Bcl-2 (Cell-free assay) Ki 0.22 μM

In Vivo Studies

Using Adooq A10665, weekly obatoclax plus TAK-228 prolonged median survival from 34 to 55 days in CHLA06 orthotopic AT/RT xenografts and from 29 to 44.5 days in BT37 xenografts. Obatoclax was given orally at 10 mg/kg in CHLA06 and intraperitoneally at 6 mg/kg in BT37; TAK-228 was given orally at 6 mg/kg in both. These are combination effects in mice. Some tumors continued to progress, and the authors identified limited durability as a study limitation. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

CHLA06 orthotopic AT/RT combination survival

Animal study · 4–6-week-old female Nu/Nu mice bearing CHLA06 orthotopic AT/RT xenografts [1]

Combination treatment prolonged median survival relative to vehicle. Results are specific to combination therapy; tumors were not uniformly controlled and responses were not generally durable.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Overall survivalMedian survival 34 days (vehicle) to 55 days (combination)[1]

Conditions shared by the study groups

Treatment course
Started day 4 after implantation; total dosing course not specified in read Methods.
Vehicle
Obatoclax: PBS, 30% PEG400, 0.5% Tween-80, 5% propylene glycol; TAK-228: 5% methylcellulose.
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Vehicle control
Vehicle only		Vehicle and both single-agent groups in the same experimentMedian survival 34 days[1]
Obatoclax alone
10 mg/kg		Vehicle and both single-agent groups in the same experimentComparator shown in Figure 8; no exact single-agent median extracted.[1]
TAK-228 alone
6 mg/kg		Vehicle and both single-agent groups in the same experimentComparator shown in Figure 8; no exact single-agent median extracted.[1]
Obatoclax plus TAK-228
10 mg/kg obatoclax + 6 mg/kg TAK-228		Vehicle and both single-agent groups in the same experimentMedian survival 55 days; prolonged versus vehicle[1]
Vehicle control
Model: 4–6-week-old female Nu/Nu mice bearing CHLA06 orthotopic AT/RT xenografts
Route: Vehicle-only administration route not separately specified in the read survival Methods.
Frequency: Vehicle-only schedule not separately specified in the read survival Methods.
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
Obatoclax alone
Model: 4–6-week-old female Nu/Nu mice bearing CHLA06 orthotopic AT/RT xenografts
Route: oral
Frequency: Once weekly for active drugs
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
TAK-228 alone
Model: 4–6-week-old female Nu/Nu mice bearing CHLA06 orthotopic AT/RT xenografts
Route: oral
Frequency: Once weekly for active drugs
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
Obatoclax plus TAK-228
Model: 4–6-week-old female Nu/Nu mice bearing CHLA06 orthotopic AT/RT xenografts
Route: oral obatoclax; oral TAK-228
Frequency: Once weekly for active drugs
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
Methods and source locations

Compound reported in the paper: Obatoclax; Compound label in the paper: Obatoclax

Published A10665 experiment; no validation of current Adooq lots.

Results: Combination therapy improves survival; Figure 8A; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Overall survival: Author-reported medians; Figure 8 caption: p < 0.05 versus vehicle, log-rank test. Methods report 10 mice treated per group. — Results: Combination therapy improves survival; Figure 8A and caption; Survival studies Methods

Vehicle control · Results: Combination therapy improves survival; Figure 8A; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Obatoclax alone · Results: Combination therapy improves survival; Figure 8A; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

TAK-228 alone · Results: Combination therapy improves survival; Figure 8A; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Obatoclax plus TAK-228 · Results: Combination therapy improves survival; Figure 8A; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

BT37 orthotopic AT/RT combination survival

Animal study · 4–6-week-old female Nu/Nu mice bearing BT37 orthotopic AT/RT xenografts [1]

Combination treatment prolonged median survival relative to vehicle. Results are specific to combination therapy; tumors were not uniformly controlled and responses were not generally durable.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Overall survivalMedian survival 29 days (vehicle) to 44.5 days (combination)[1]

Conditions shared by the study groups

Treatment course
Started day 4 after implantation; total dosing course not specified in read Methods.
Vehicle
Obatoclax: PBS, 30% PEG400, 0.5% Tween-80, 5% propylene glycol; TAK-228: 5% methylcellulose.
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Vehicle control
Vehicle only		Vehicle and both single-agent groups in the same experimentMedian survival 29 days[1]
Obatoclax alone
6 mg/kg		Vehicle and both single-agent groups in the same experimentComparator shown in Figure 8; no exact single-agent median extracted.[1]
TAK-228 alone
6 mg/kg		Vehicle and both single-agent groups in the same experimentComparator shown in Figure 8; no exact single-agent median extracted.[1]
Obatoclax plus TAK-228
6 mg/kg obatoclax + 6 mg/kg TAK-228		Vehicle and both single-agent groups in the same experimentMedian survival 44.5 days; prolonged versus vehicle[1]
Vehicle control
Model: 4–6-week-old female Nu/Nu mice bearing BT37 orthotopic AT/RT xenografts
Route: Vehicle-only administration route not separately specified in the read survival Methods.
Frequency: Vehicle-only schedule not separately specified in the read survival Methods.
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
Obatoclax alone
Model: 4–6-week-old female Nu/Nu mice bearing BT37 orthotopic AT/RT xenografts
Route: intraperitoneal
Frequency: Once weekly for active drugs
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
TAK-228 alone
Model: 4–6-week-old female Nu/Nu mice bearing BT37 orthotopic AT/RT xenografts
Route: oral
Frequency: Once weekly for active drugs
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
Obatoclax plus TAK-228
Model: 4–6-week-old female Nu/Nu mice bearing BT37 orthotopic AT/RT xenografts
Route: intraperitoneal obatoclax; oral TAK-228
Frequency: Once weekly for active drugs
Reported limits: Ten mice treated per group; analyzed survival denominators after prespecified early weight-loss exclusions not explicitly tabulated. Exact duration of dosing not specified in read Methods. SI weight data not retrieved; no broad safety claim.
Methods and source locations

Compound reported in the paper: Obatoclax; Compound label in the paper: Obatoclax

Published A10665 experiment; no validation of current Adooq lots.

Results: Combination therapy improves survival; Figure 8C; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Overall survival: Author-reported medians; Figure 8 caption: p < 0.05 versus vehicle, log-rank test. Methods report 10 mice treated per group. — Results: Combination therapy improves survival; Figure 8C and caption; Survival studies Methods

Vehicle control · Results: Combination therapy improves survival; Figure 8C; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Obatoclax alone · Results: Combination therapy improves survival; Figure 8C; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

TAK-228 alone · Results: Combination therapy improves survival; Figure 8C; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Obatoclax plus TAK-228 · Results: Combination therapy improves survival; Figure 8C; Methods: Intracranial xenograft tumors, Survival studies, Statistical analysis and Cell lines and cell culture

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 803712-79-0
Applications Bcl-2 Inhibitor
Formula C20H19N3O.CH4O3S
Molecular Weight 413.5
Synonyms GX15-070
SMILES
O=S(O)(C)=O.CC1=C(NC(C)=C1)/C=C2N=C(C3=CC4=C(N3)C=CC=C4)C=C\2OC

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 81 mg/mL (195.89 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
30% PEG400+0.5% Tween80+5% propylene glycol

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Parkhurst A, Wang SZ, Findlay TR, et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors Cell death & disease (2022). PMID: 35484114 DOI: 10.1038/s41419-022-04868-9 Source material

Publications

4 publications citing this product

  1. Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
  2. Silva S, .et al. , Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
  3. Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
  4. P Geserick, .et al. , Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795

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