PROTAC BCR-ABL1 ligand 1

Name: PROTAC BCR-ABL1 ligand 1
Brand: MedChemExpress
SKU: HY-130297
Rating: 4.5 (1 reviews)

Cat. No.: HY-130297 Purity: 99.17%: Data Sheet
COA

SDS
Handling Instructions
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PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.

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

PROTAC BCR-ABL1 ligand 1 Chemical Structure

CAS No. : 2489876-34-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
250 mg	Get quote	Estimated Time of Arrival: December 31
500 mg	Get quote
1 g	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

GMB-475 (0-10 μM) exhibits cell proferation with IC₅₀ values of 1.11,1.98,0.37 μM for BCR-ABL1 WT, T315I, G250E cells, respectively^[1].
GMB-475 (0-30 μM) induces the degradation of BCR-ABL1 and c-ABL1 with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion in the context of both K562 and Ba/F3 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	K562 and Ba/F3 cells
Concentration:	0-30 μM
Incubation Time:
Result:	Decreased p-STAT5 expression.

Molecular Weight

347.29

Formula

C₁₇H₁₂F₃N₃O₂

CAS No.

2489876-34-6

Appearance

Solid

Color

Light brown to gray

SMILES

OC1=CC=C(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (359.93 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	2.8794 mL	14.3972 mL	28.7944 mL
5 mM	0.5759 mL	2.8794 mL	5.7589 mL
10 mM	0.2879 mL	1.4397 mL	2.8794 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
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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

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In Vivo Dissolution Calculator

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Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.17%

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Data Sheet (270 KB) SDS (393 KB)

COA (245 KB) HNMR (278 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation. Cancer Res. 2019 Sep 15;79(18):4744-4753. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8794 mL	14.3972 mL	28.7944 mL	71.9859 mL
	5 mM	0.5759 mL	2.8794 mL	5.7589 mL	14.3972 mL
	10 mM	0.2879 mL	1.4397 mL	2.8794 mL	7.1986 mL
	15 mM	0.1920 mL	0.9598 mL	1.9196 mL	4.7991 mL
	20 mM	0.1440 mL	0.7199 mL	1.4397 mL	3.5993 mL
	25 mM	0.1152 mL	0.5759 mL	1.1518 mL	2.8794 mL
	30 mM	0.0960 mL	0.4799 mL	0.9598 mL	2.3995 mL
	40 mM	0.0720 mL	0.3599 mL	0.7199 mL	1.7996 mL
	50 mM	0.0576 mL	0.2879 mL	0.5759 mL	1.4397 mL
	60 mM	0.0480 mL	0.2400 mL	0.4799 mL	1.1998 mL
	80 mM	0.0360 mL	0.1800 mL	0.3599 mL	0.8998 mL
	100 mM	0.0288 mL	0.1440 mL	0.2879 mL	0.7199 mL