HEMTAC CDK4/6 degrader 1

Name: HEMTAC CDK4/6 degrader 1
Brand: MedChemExpress
SKU: HY-152263
Rating: 4.5 (1 reviews)

Cat. No.: HY-152263 Purity: 98.18%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a K_d value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 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.

HEMTAC CDK4/6 degrader 1 Chemical Structure

CAS No. : 2821803-61-4

Size	Stock	Quantity
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	Get quote
200 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a K_d value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer^[1]. HEMTAC CDK4/6 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^[1]

CDK4

CDK6

In Vitro

HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) induces CDK4 and CDK6 degradation in the treated B16F10 cells with a DC₅₀ value (the drug concentration that results in 50% protein degradation) of approximately 26 and 19 nM and a D_max (maximal percent degradation) of 88 and 92%, respectively^[1].
HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) has anti-proliferative activity against a broad range of human cancer cell lines^[1].
HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) induces B16F10 cells to undergo apoptosis in a dose-dependent manner and arrests cell cycle at G0/G1 phase^[1].

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

Cell Viability Assay^[1]

Cell Line:	B16F10, A375, HepG2, MDA-MB-231, and A549 cells
Concentration:	0.01-100 μM
Incubation Time:	72 hours
Result:	Inhibited cell growth in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	B16F10 cells
Concentration:	250 nM
Incubation Time:	48 hours
Result:	Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:	B16F10 cells
Concentration:	250 nM
Incubation Time:	48 hours
Result:	Increased the amount of B16F10 cells in the G0/G1 phase.

Western Blot Analysis^[1]

Cell Line:	B16F10 cells
Concentration:	0.01, 0.05, 0.1, 0.5, and 1 μM
Incubation Time:	24 hours
Result:	Induced CDK4/6 degradation in a dose-dependent manner.

In Vivo

HEMTAC CDK4/6 degrader 1 (compound 26; 20 and 40 mg/kg; i.p.; daily, for 15 d) has antitumor efficacy in C57BL/6J mice bearing B16F10 melanoma xenografts^[1].

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

Animal Model:	C57BL/6J mice bearing B16F10 melanoma xenografts^[1]
Dosage:	20 and 40 mg/kg
Administration:	intraperitoneal injection; daily, for 15 days
Result:	Inhibited tumor growth and resulted in fewer CDK4/6-positive cells and led to much more necrosis.

Molecular Weight

953.49

Formula

C₄₈H₅₃ClN₁₆O₄

CAS No.

2821803-61-4

Appearance

Solid

Color

Light yellow to green yellow

SMILES

ClC1=C2C(N(C=C2C#CCCN3C=C(N=N3)CNC(CN4CCN(C5=CN=C(C=C5)NC6=NC=C(C7=N6)C(C)=C(C(N7C8CCCC8)=O)C(C)=O)CC4)=O)CC9=NC=C(C(OC)=C9C)C)=NC(N)=N1

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 : 100 mg/mL (104.88 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	1.0488 mL	5.2439 mL	10.4878 mL
5 mM	0.2098 mL	1.0488 mL	2.0976 mL
10 mM	0.1049 mL	0.5244 mL	1.0488 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
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 Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.18%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (245 KB) HNMR (140 KB) RP-HPLC (171 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Li Z, et, al. Targeted Protein Degradation Induced by HEMTACs Based on HSP90. J Med Chem. 2023 Jan 12;66(1):733-751. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.0488 mL	5.2439 mL	10.4878 mL	26.2195 mL
	5 mM	0.2098 mL	1.0488 mL	2.0976 mL	5.2439 mL
	10 mM	0.1049 mL	0.5244 mL	1.0488 mL	2.6219 mL
	15 mM	0.0699 mL	0.3496 mL	0.6992 mL	1.7480 mL
	20 mM	0.0524 mL	0.2622 mL	0.5244 mL	1.3110 mL
	25 mM	0.0420 mL	0.2098 mL	0.4195 mL	1.0488 mL
	30 mM	0.0350 mL	0.1748 mL	0.3496 mL	0.8740 mL
	40 mM	0.0262 mL	0.1311 mL	0.2622 mL	0.6555 mL
	50 mM	0.0210 mL	0.1049 mL	0.2098 mL	0.5244 mL
	60 mM	0.0175 mL	0.0874 mL	0.1748 mL	0.4370 mL
	80 mM	0.0131 mL	0.0655 mL	0.1311 mL	0.3277 mL
	100 mM	0.0105 mL	0.0524 mL	0.1049 mL	0.2622 mL