2. Epigenetics Apoptosis
  3. Epigenetic Reader Domain Apoptosis
  4. TDI-11055

TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC50 values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia.

For research use only. We do not sell to patients.

TDI-11055

TDI-11055 Chemical Structure

CAS No. : 3057216-63-1

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10 mM * 1 mL in DMSO
ready for reconstitution
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TDI-11055 Related Antibodies

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Description

TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC50 values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia[1][2].

IC50 & Target[1]

ENL YEATS domain

50 nM (IC50)

ENL YEATS domain

119 nM (Kd)

AF9 YEATS domain

70 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MV4-11 IC50
0.1 μM
Compound: 8; TDI-11055
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth by CellTiter-Glo Luminescent Cell Viability Assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth by CellTiter-Glo Luminescent Cell Viability Assay
[PMID: 38628784]
In Vitro

TDI-11055 binds directly to the ENL YEATS domain with a Kd of 119 nM[1].
TDI-11055 (5 μM; 24 hours) displaces ENL from chromatin at target genes in MOLM-13 cells without reducing ENL protein levels[1].
TDI-11055 (8 days) potently inhibits proliferation of MLL-r and NPM1-mutated leukemia cell lines with IC50 values ranging from 0.27 to 7.2 μM, but has minimal effects on non-MLL-r cell lines[1].
TDI-11055 (1-10 μM; 72 h) inhibits the growth of MV4;11 and OCI-AML3 cells, accompanied by a slowing of cell cycle progression and a mild increase in apoptosis[1].
TDI-11055 (1-10 μM; ~7 days) impairs clonogenic potential of MLL-r MV4;11 and NPM1-mutated OCI-AML3 cells but not non-MLL-r HL60 or K562 cells[1].
TDI-11055 (5 μM; 24 hours) suppresses ENL-dependent oncogenic gene expression programs in MV4;11 cells, including MYC and HOXA cluster genes, and induces myeloid differentiation[1].
TDI-11055 (5 μM; 30 minutes, 2 hours, or 24 hours) rapidly displaces ENL from chromatin, reducing SEC/P-TEFb and DOT1L occupancy and Pol II S2P levels at top ENL-bound genes in MV4;11 cells[1].
TDI-11055 (1-10 μM; ~2 weeks) impairs clonogenic potential of MLL-r and NPM1-mutated primary AML samples but not normal hematopoietic cells[1].
TDI-11055 (8-day) inhibits the growth of MV4;11 AML cells with an IC50 of 0.10 μM in a viability assay[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TDI-11055 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human leukemia cell lines (MV4;11, MOLM-13, ML2, OCI-AML2, OCI-AML3, HL60, K562, U937, Jurkat)
Concentration: 1-100 μM
Incubation Time: 8 days
Result: Inhibited proliferation of MLL-rearranged (MLL-r) cell lines MV4;11 (IC₅₀ = 0.27 μM), MOLM-13 (IC₅₀ = 0.77 μM), OCI-AML2 (IC₅₀ = 1.79 μM), ML2 (IC₅₀ = 7.2 μM) and NPM1-mutated OCI-AML3 (IC₅₀ = 0.51 μM); exerted minimal effects on non-MLL-r cell lines HL60 (IC₅₀ > 30 μM), K562 (IC₅₀ > 30 μM), U937 (IC₅₀ = 23 μM), Jurkat (IC₅₀ > 30 μM).

Apoptosis Analysis[1]

Cell Line: MV4;11 and OCI-AML3 cells
Concentration: 1 μM, 10 μM
Incubation Time: 72 h
Result: Increaseed the apoptosis percentage of MV4;11 and OCI-AML3.
Parmacokinetics
Species Dose Route T1/2 F CL Vss_obs AUC0-24
Mice[1] 30 mg/kg p.o. 2.7 h / / / /
Mice[1] 50 mg/kg p.o. 2.8 h / / / /
Mice[1] 100 mg/kg p.o. 5.0 / / / /
Rat[2] 2 mg/kg i.v. 1.54 h / 108 mL/min/kg 7.3 L/kg 314 ng·h/mL
Rat[2] 10 mg/kg p.o. / 31 % / / /
In Vivo

TDI-11055 (100-200 mg/kg; p.o.; b.i.d.; 8 days) inhibits tumor growth and downregulates key oncogenic genes in MV4;11 subcutaneous AML xenografts[1].
TDI-11055 (200 mg/kg; p.o.; q.d.; 28 days) reduces leukemia burden and prolongs survival in disseminated MV4;11 AML xenografts[1].
TDI-11055 (200 mg/kg; p.o.; q.d.; 28 days) reduces leukemia burden in MLL-r PDX-6315 AML xenografts[1].
TDI-11055 (200 mg/kg; p.o.; q.d.; 28 days) prolongs survival in OCI-AML3 NPM1-mutated AML xenografts[1].
TDI-11055 (200 mg/kg; p.o.; q.d.; 28 days) reduces leukemia burden in NPM1-mutated PDX-3055 AML xenografts[1].
TDI-11055 (200 mg/kg; p.o.; q.d. or b.i.d. (5 days on/2 days off); 28 days) reduces leukemia burden and prolongs survival in MLL-r PDX-2263 AML xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (female, 6-8 weeks old) bearing MV4;11 subcutaneous transplantation model[1].
Dosage: 100 mg/kg; 200 mg/kg
Administration: p.o.; b.i.d.; 8 days
Result: Significantly inhibited tumor growth; reduced mRNA expression of MYC, HOXA9, MEIS1, and MYB in tumors.
Animal Model: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) (female, 6-8 weeks old)[1]
Dosage: 200 mg/kg
Administration: p.o.; q.d.; 28 days
Result: Reduced leukemia burden (human CD45+ cells in peripheral blood); prolonged median survival from 37 to 63 days (70% increase).
Reduced leukemia burden (human CD45+ cells in peripheral blood, bone marrow, and spleen).
Prolonged median survival.
Significantly reduced leukemia burden (human CD45+ cells in bone marrow).
Animal Model: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) (female, 6-8 weeks old)[1]
Dosage: 200 mg/kg
Administration: p.o.; q.d. (for 28 days); b.i.d. (5 days on/2 days off for 28 days)
Result: Reduced leukemia burden (human CD45+ cells in peripheral blood); prolonged median survival from 32 to 49 days (53% increase)
Molecular Weight

388.47

Formula

C22H24N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1CCCN1CC2=CC3=C(N2)C=C(N=C3)NC(C4=CC=C5C(C=NN5C)=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (257.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5742 mL 12.8710 mL 25.7420 mL
5 mM 0.5148 mL 2.5742 mL 5.1484 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.44 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5742 mL 12.8710 mL 25.7420 mL 64.3550 mL
5 mM 0.5148 mL 2.5742 mL 5.1484 mL 12.8710 mL
10 mM 0.2574 mL 1.2871 mL 2.5742 mL 6.4355 mL
15 mM 0.1716 mL 0.8581 mL 1.7161 mL 4.2903 mL
20 mM 0.1287 mL 0.6436 mL 1.2871 mL 3.2178 mL
25 mM 0.1030 mL 0.5148 mL 1.0297 mL 2.5742 mL
30 mM 0.0858 mL 0.4290 mL 0.8581 mL 2.1452 mL
40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6089 mL
50 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2871 mL
60 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0726 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8044 mL
100 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6436 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TDI-110553057216-63-1TDI11055TDI 11055Epigenetic Reader DomainApoptosisMLL rearrangementsENL YEATS domainENLcrotonyl markshistone tailsacetyl markschromatinacylated histonesAMLNPM1 mutationsInhibitorinhibitorinhibit

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