Referencia número: HY-13024

Rebastinib

(Synonyms: DCC-2036)

13 Cited Publications

Revisión del cliente

Based on 13 publication(s) in Google Scholar

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.

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Pureza: 99.74%
No. CAS: 1020172-07-9
Fòrmula: C₃₀H₂₈FN₇O₃
Peso molecular:553.59

Almacenamiento:

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

Rebastinib Chemical Structure

No. CAS: 1020172-07-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (13)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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]

Ver todos los productos específicos de isoformas Bcr-Abl :

Abl
Bcr-Abl

Ver todos los productos específicos de isoformas Src :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	120 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	127 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
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	13 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	14 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	150 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
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]
BaF3	IC₅₀	19 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	24 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	3500 nM Compound: DCC-2036	Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	36 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	39 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	5.4 nM Compound: DCC-2036	Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	51 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	56 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	6 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	81 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
BaF3	IC₅₀	98 nM Compound: DCC-2036	Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 21481795]
K562	IC₅₀	5.5 nM Compound: DCC-2036	Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay	[PMID: 21481795]

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1020172-07-9
Appearance Solid
Peso molecular 553.59
Fòrmula C₃₀H₂₈FN₇O₃
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
Synonyms

DCC-2036
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (13)

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Journal Impact Factor

Nat Commun

Caveolae-mediated Tie2 signaling contributes to CCM pathogenesis in a brain endothelial cell-specific Pdcd10-deficient mouse model. [Abstract]

2021 Jan 25;12(1):504. PMID: 33495460

Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]

Rebastinib (1 μM) blunted increased EC sprouting and enlarged lumen formation induced by CCM3 knockdown.

Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]

Rebastinib (10 μg/g; s.c.; 11 d) diminished the CCM lesions induced by Ccm3 deletion as visualized by whole-brain imaging and H&E staining compared to vehicle treatment in Pdcd10^BECKO mice.

Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]

Rebastinib (10 μg/g; s.c.; once daily for 11 d) normalized the NG2⁺ pericyte coverage of CD31⁺ microvessels in Pdcd10^BECKO mice.

Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]

Rebastinib (10 μg/g; s.c.; once daily for 11 d) caussed very fewer CCM lesions in brain of Pdcd10^BECKO mice compared to vehicle group even at age of 2 months.

Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]

Rebastinib (10 μg/g; s.c.; 11 d) increased pericyte density and diminished pericyte-free caverns in Pdcd10^BECKO mice.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Clin Invest

Vessels encapsulating tumor clusters promote noninvasive metastasis of hepatocellular carcinoma by shaping an immunosuppressive microenvironment. [Abstract]

2026 Jan 6;136(4):e193758. PMID: 41493808
J Exp Clin Cancer Res

CDK16 promotes the progression and metastasis of triple-negative breast cancer by phosphorylating PRC1. [Abstract]

2022 Apr 21;41(1):149. PMID: 35449080
Brain

Three-dimensional tissue engineered skeletal muscle modelling facioscapulohumeral muscular dystrophy. [Abstract]

2025 May 13;148(5):1723-1739. PMID: 39556762
J Exp Med

TIE2 links MEKK3-KLF2/4 and PI3K signaling in cerebral cavernous malformation. [Abstract]

2026 May 4;223(5):e20251374. PMID: 41891922
J Med Chem

Conformational analysis of the DFG-out kinase motif and biochemical profiling of structurally validated type II inhibitors. [Abstract]

2015 Jan 8;58(1):466-79. PMID: 25478866
J Cell Sci

LRRK2 mutations block NCOA4 trafficking upon iron overload leading to ferroptotic death. [Abstract]

2026 May 28:jcs.264977. PMID: 42206576
Anticancer Drugs

AZD7762 induces CRBN dependent BAG3 degradation through ubiquitin-proteasome pathway. [Abstract]

2024 Jan 1;35(1):46-54. PMID: 37449977
Res Sq

2025 Sep 1.
bioRxiv

2025 August 23.
University of Washington

2025.
Patent

US20170349880A1.

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

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In Vivo:

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

Stock Solution Working Solution

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% (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.

In Vivo Dissolution Calculator

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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).

Working solution concentration: 0.22 mg/mL

Protocolo

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].

MedChemExpress (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).

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (284 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Rebastinib

13 Cited Publications

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Rebastinib

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Publications Citing Use of MedChemExpress (MCE) Rebastinib

Ver todos los productos específicos de isoformas Bcr-Abl

Ver todos los productos específicos de isoformas Src

Actividad biológica

Chemical Information

Publications (13)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Rebastinib Related Classifications

HY-13024 Related Classifications