Rebastinib (Synonyms: DCC-2036)

Name: Rebastinib
Brand: MedChemExpress
SKU: HY-13024
Rating: 5.0 (6 reviews)

Cat. No.: HY-13024 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1^WT and Abl1^T315I with IC₅₀s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.

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

Rebastinib Chemical Structure

CAS No. : 1020172-07-9

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Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 94	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 94	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 319	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE Rebastinib

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 0.75±0.11 nM (ABL1^WT), 2±0.3 nM (FLT3), 4±0.3 nM (KDR), 6±0.3 nM (TIE2), 34±6 nM (SRC)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	13 nM Compound: DCC-2036	Antiproliferative activity against mouse BAF3 cells harboring wild type BCR-ABL measured after 72 hrs by MTT assay Antiproliferative activity against mouse BAF3 cells harboring wild type BCR-ABL measured after 72 hrs by MTT assay	[PMID: 35551036]
BaF3	IC₅₀	19 nM Compound: DCC-2036	Antiproliferative activity against mouse BAF3 cells harboring BCR-ABL T315I mutant measured after 72 hrs by MTT assay Antiproliferative activity against mouse BAF3 cells harboring BCR-ABL T315I mutant measured after 72 hrs by MTT assay	[PMID: 35551036]

In Vitro

Rebastinib potently (IC₅₀ 0.82 nM) inhibits u-ABL1^native, which is thought to exist predominantly in the inactive type II conformation. In addition, Rebastinib also strongly inhibits p-ABL1^native (IC₅₀ 2 nM), which more readily adopts an active, Type I conformation^[1].
Rebastinib potently inhibits both u-ABL1^T315I (IC₅₀ 5 nM) and p-ABL1^T315I (IC₅₀ 4 nM), both of which exist predominately in the Type I conformation due to stabilization of an activating hydrophobic spine by the T315I mutation^[1].
In addition to ABL1, Rebastinib also inhibits the SRC family kinases LYN, SRC, FGR, and HCK, and PDGFRα, and PDGFRβ with IC₅₀ of 29±1, 34±6, 38±1, 40±1, 70±10 and 113±10 nM, respectively. Notably, Rebastinib spared c-KIT (IC₅₀ 481 nM)^[1].
Rebastinib effectively inhibits the proliferation of Ba/F3 cells expressing native BCR-ABL1^native (IC₅₀ 5.4 nM). Rebastinib also inhibits proliferation of the Ph⁺ cell line K562 (IC₅₀ 5.5 nM)^[1].
Rebastinib also inhibits proliferation of several common TKI-resistant mutants of BCR-ABL1, including G250E, Q252H, Y235F, E255K, V299L, F317L, and M351T, at IC₅₀s ranging from 6-150 nM. Rebastinib effectively inhibits autophosphorylation of BCR-ABL1^native (IC₅₀ 29 nM) and BCR-ABL1^T315I (IC₅₀ 18 nM), as well as the phosphorylation of STAT5 in both cell lines (IC₅₀ 28 nM and 13 nM, respectively)^[1].

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

In Vivo

A single dose of Rebastinib (DCC-2036; oral; 100 mg/kg) affords circulating plasma levels that exceeds 12 μM for up to 24 hours, and effectively inhibits BCR-ABL1 signaling for up to 8 hours in Ba/F3-BCR-ABL1^T315I leukemia cells isolated from BM and spleen of tumor-bearing mice^[1].
Treatment of mice bearing Ba/F3-BCR-ABL1^T315I leukemia cells with Rebastinib at 100 mg/kg once daily by oral gavage significantly prolonged their survival, while STI571 at 100 mg/kg twice daily is ineffective^[1].
In this aggressive allograft model, Rebastinib is as effective for treatment of BCR-ABL^T315I leukemia as STI571 at 100 mg/kg twice daily in BCR-ABL1^native leukemia, and reduces the leukemia cell burden in the spleens of treated mice^[1].

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

Clinical Trial

Molecular Weight

553.59

Formula

C₃₀H₂₈FN₇O₃

CAS No.

1020172-07-9

Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C)C1=NN(C(NC(NC2=C(F)C=C(OC3=CC(C(NC)=O)=NC=C3)C=C2)=O)=C1)C4=CC=C5C(C=CC=N5)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (90.32 mM; ultrasonic and warming and heat to 80°C; 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	1.8064 mL	9.0320 mL	18.0639 mL
5 mM	0.3613 mL	1.8064 mL	3.6128 mL
10 mM	0.1806 mL	0.9032 mL	1.8064 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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).

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

Purity: 99.91%

Select Batch:

Data Sheet (284 KB) SDS (251 KB)

COA (254 KB) HNMR (207 KB) LCMS (120 KB)

Handling Instructions (2659 KB)

References

[1]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011, 19(4), 556-568. [Content Brief]

Cell Assay ^[1]	Ba/F3 cells (3×10³ cells/well) or primary Ph+ leukemia cells (5×10⁴ cells/well) are plated in triplicate in 96-well plates containing test compounds (e.g., Rebastinib (DCC-2036)). After 72h, viable cells are quantified by resazurin or MTT assay. Results represent an average of at least three independent experiments^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Ba/F3 cells (1×10⁶) transformed to interleukin-3 independence by transduction with either BCR-ABL1^native or BCR-ABL1^T315I retrovirus are injected intravenously into syngeneic Balb/c recipients. Beginning day 3 post-injection, mice are treated with STI571 (100 mg/kg in water twice daily via oral gavage) or with Rebastinib (DCC-2036) (100 mg/kg in 0.5% CMC/1% Tween-80, once daily via oral gavage) or with vehicle (0.5% CMC/1% Tween-80) alone. For induction of CML-like leukemia, bone marrow (BM) from male Balb/c donor mice is harvested 4d after intravenous administration of 150 mg/kg 5-FU, transduced with BCR-ABL1^T315I retrovirus, and 5×10⁵ cells injected intravenously into sublethally irradiated (400 cGy) Balb/c recipients. Beginning at d5 post-transplant, cohorts are treated once daily by oral gavage with vehicle alone, or Rebastinib (DCC-2036) at 100 mg/kg. For induction of B-cell acute lymphoblastic leukemia, BM from donors not pretreated with 5-FU is transduced once with BCR-ABL1^T315I retrovirus and 1×10⁶ cells injected into sublethally irradiated Balb/c recipients. Beginning at d8 post-transplant, cohorts are treated twice daily by oral gavage with vehicle alone, with Rebastinib (DCC-2036) at 60 mg/kg, with STI571 at 100 mg/kg (in water), or with BMS-354825 at 10 mg/kg (in 80 mM citric acid pH 3.1). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011, 19(4), 556-568. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8064 mL	9.0320 mL	18.0639 mL	45.1598 mL
	5 mM	0.3613 mL	1.8064 mL	3.6128 mL	9.0320 mL
	10 mM	0.1806 mL	0.9032 mL	1.8064 mL	4.5160 mL
	15 mM	0.1204 mL	0.6021 mL	1.2043 mL	3.0107 mL
	20 mM	0.0903 mL	0.4516 mL	0.9032 mL	2.2580 mL
	25 mM	0.0723 mL	0.3613 mL	0.7226 mL	1.8064 mL
	30 mM	0.0602 mL	0.3011 mL	0.6021 mL	1.5053 mL
	40 mM	0.0452 mL	0.2258 mL	0.4516 mL	1.1290 mL
	50 mM	0.0361 mL	0.1806 mL	0.3613 mL	0.9032 mL
	60 mM	0.0301 mL	0.1505 mL	0.3011 mL	0.7527 mL
	80 mM	0.0226 mL	0.1129 mL	0.2258 mL	0.5645 mL

Rebastinib Related Classifications

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:

Rebastinib1020172-07-9DCC-2036DCC2036DCC 2036Bcr-AblFLT3SrcApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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Rebastinib (Synonyms: DCC-2036)

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Rebastinib Related Antibodies

6 Publications Citing Use of MCE Rebastinib

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Src Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Rebastinib Related Antibodies

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Complete Stock Solution Preparation Table

Rebastinib Related Classifications

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