PROTAC BCR-ABL Degrader-2

Cat. No.: HY-180967: Data Sheet Handling Instructions
FAQs
Technical Support

PROTAC BCR-ABL Degrader-2 is a selective Bcr-Abl^T315 PROTAC degrader with a DC₅₀ of 108.7 nM in Ba/F3 Bcr-Abl^T315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research.
(Pink: Bcr-Abl ligand (HY-15666); Blue: Cereblon ligand (HY-10984); Black: linker).

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

PROTAC BCR-ABL Degrader-2 Chemical Structure

CAS No. : 2703834-25-5

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Bcr-Abl Isoform Specific Products:

View All Isoforms

Abl Bcr-Abl

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

PROTAC BCR-ABL Degrader-2 is a selective Bcr-Abl^T315 PROTAC degrader with a DC₅₀ of 108.7 nM in Ba/F3 Bcr-Abl^T315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research^[1]^[2]. (Pink: Bcr-Abl ligand (HY-15666); Blue: Cereblon ligand (HY-10984); Black: linker).

In Vitro

PROTAC BCR-ABL Degrader-2 (Compound 7o) (72 h) against K562, Ba/F3 Bcr-Abl^lT315I and Ba/F3 Bcr-Abl^WT with IC₅₀s of 7.7, 26.8 and 4.2 nM^[1].
PROTAC BCR-ABL Degrader-2 (0-300 nM) significantly decreases the level of Bcr-AblT315I protein with a DC₅₀ = 108.7 nM in Ba/F3 Bcr-Abl^T315I cells^[1].
PROTAC BCR-ABL Degrader-2 (0-300 nM, 0-48 h) induces Bcr-Abl^T315I protein level mediated by CRBN E3 ubiquitin pathway while appeared a “hook” effect in Bcr-Abl^lT315I cell^[1].

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

Western Blot Analysis^[1]

Cell Line:	Ba/F3 Bcr-Abl^T315I and K562 cells
Concentration:	100 nM
Incubation Time:	0, 1, 2, 4, 6, 8, 10, 12, 24, 36 and 48 h
Result:	Caused the degradation of Bcr-Abl^T315I protein in a time-dependent manner. Reduced Bcr-Abl^T315I protein level substantially after 6h treatment while appeared a “hook” effect during 8-10h treatment. Observed the maximum degradation after24h treatment. Displayed a different trend for reducing Bcr-Abl^WT in K562cells with substantially reduction after 36h treatment (this different might be associated with the different states of E3 ligase in Ba/F3Bcr-Abl^T315I and K562 cells.).

Immunofluorescence^[1]

Cell Line:	MG132 (HY-13259) (20 ) Ba/F3 Bcr-Abl^T315I cells
Concentration:	100 and 300 nM
Incubation Time:	24 h
Result:	Induced Bcr-Abl^T315I degradation rescuing by MG132.

In Vivo

PROTAC BCR-ABL Degrader-2 (compound 7o) (20 mg/kg, i.p., once) shows high plasma concentrations maintained over 48 h in ICR mice^[1].
PROTAC BCR-ABL Degrader-2 (10-20 mg/kg, i.p., once every two days for 14 days) displays significant anti-cancer activity and safety in the Ba/F3 Bcr-Abl^T315I mice xenograft models^[1].

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

Animal Model:	Ba/F3 cells expressing Bcr-Abl^T315I (2 x 10⁶ cells/0.1 mL) induced-CB17-SCID mice ^[1]
Dosage:	10 or 20 mg/kg
Administration:	i.p., once every two days for 14 days
Result:	Obviously sup pressed the growth of Ba/F3 Bcr-Abl^T315I xenograft tumor with a tumor growth inhibition (TGI) value of 90.8% at the dose of 20 mg/kg. Induced the Bcr-Abl^T315I degradation and apoptosis. Resulted no mortality or significant body weight loss.

Molecular Weight

901.93

Formula

C₄₈H₄₆F₃N₉O₆

CAS No.

2703834-25-5

SMILES

O=C(C1=CC=C(C)C(C#CC2=CC3=C(NN=C3)N=C2)=C1)NC4=CC=C(CN5CCN(CCCCCCC(NC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)CC5)C(C(F)(F)F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Jiang L, et al. Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Acta Pharm Sin B. 2021 May;11(5):1315-1328. [Content Brief]

[2]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]