PROTAC BTK Degrader-1

Name: PROTAC BTK Degrader-1
Brand: MedChemExpress
SKU: HY-147943
Rating: 4.5 (1 reviews)

Cat. No.: HY-147943 Purity: 98.87%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC₅₀ value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

PROTAC BTK Degrader-1 Chemical Structure

CAS No. : 2801715-13-7

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	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

PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC₅₀ value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth^[1]. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

IC₅₀: 34.51 nM (BTK WT), 64.56 nM (BTK-481S)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
JeKo-1	IC₅₀	104.69 nM Compound: C13	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
JeKo-1	IC₅₀	708.2 nM Compound: C13	Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
OCI-Ly10	IC₅₀	5.9 nM Compound: C13	Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
TMD8	IC₅₀	4.7 nM Compound: C13	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]

In Vivo

PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model^[1].
Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice^[1].

	PO (100 mg/kg)	IV (2 mg/kg)
T_max (h)	1.00
T_1/2 (h)	8.3	3.7
C_max (ng/mL)	3089
AUC_0-t (ng/mL·h)	16,894	2827
AUC_0-∞ (ng/mL·h)	17,070	2845
Vd_SS (L/kg)		3.1
CL (mL/min/kg)		11.7
MRT (h)		4.5
F (%)	12

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

Animal Model:	OCI-ly10 xenograft mouse model^[1]
Dosage:	10 and 30 mg/kg
Administration:	PO, bid, for 17 days
Result:	Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.

Molecular Weight

749.86

Formula

C₄₃H₄₃N₉O₄

CAS No.

2801715-13-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1)C(CCC1=O)N(C2=O)CC3=C2C=CC(C#CCN4CCC(CC4)N5CCC(CC5)N6N=C(C7=C(N=CN=C76)N)C8=CC=C(C=C8)OC9=CC=CC=C9)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (133.36 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	1.3336 mL	6.6679 mL	13.3358 mL
5 mM	0.2667 mL	1.3336 mL	2.6672 mL
10 mM	0.1334 mL	0.6668 mL	1.3336 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.87%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (253 KB) HNMR (311 KB) RP-HPLC (262 KB) LCMS (145 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang J, et al. Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma. J Med Chem. 2022 Jun 7. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.3336 mL	6.6679 mL	13.3358 mL	33.3396 mL
	5 mM	0.2667 mL	1.3336 mL	2.6672 mL	6.6679 mL
	10 mM	0.1334 mL	0.6668 mL	1.3336 mL	3.3340 mL
	15 mM	0.0889 mL	0.4445 mL	0.8891 mL	2.2226 mL
	20 mM	0.0667 mL	0.3334 mL	0.6668 mL	1.6670 mL
	25 mM	0.0533 mL	0.2667 mL	0.5334 mL	1.3336 mL
	30 mM	0.0445 mL	0.2223 mL	0.4445 mL	1.1113 mL
	40 mM	0.0333 mL	0.1667 mL	0.3334 mL	0.8335 mL
	50 mM	0.0267 mL	0.1334 mL	0.2667 mL	0.6668 mL
	60 mM	0.0222 mL	0.1111 mL	0.2223 mL	0.5557 mL
	80 mM	0.0167 mL	0.0833 mL	0.1667 mL	0.4167 mL
	100 mM	0.0133 mL	0.0667 mL	0.1334 mL	0.3334 mL