A-1331852

Name: A-1331852
Brand: MedChemExpress
SKU: HY-19741
Rating: 5.0 (34 reviews)

Cat. No.: HY-19741 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

A-1331852 is an orally available BCL-XL selective inhibitor with a K_i of less than 10 pM.

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

A-1331852 Chemical Structure

CAS No. : 1430844-80-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 209	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 209	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 228	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 468	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 744	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1320	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 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 34 publication(s) in Google Scholar

33 Publications Citing Use of MCE A-1331852

Cell Viability Assay

: A-1331852 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jun 8;11(6):443. [Abstract]; In A375 cells, knockdown (KD) of MCL1 (shMCL1), BCL2 (shBCL2), BCLW (shBCLW), and BCLXL (shBCLXL) lines are created by shRNA technology. shMCL1 (in presence of ABT-263 or A-1331852) shows significant reduction in cell viability during 48 h drug treatment.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms

Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

A-1331852 is an orally available BCL-XL selective inhibitor with a K_i of less than 10 pM.

IC₅₀ & Target^[1]

Bcl-xL

0.01 nM (Ki)

Bcl-W

4 nM (Ki)

Bcl-2

6 nM (Ki)

Mcl-1

142 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
MOLT-4	EC₅₀	6 nM Compound: 33; A-1331852	Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay	[PMID: 26988306]
MOLT-4	EC₅₀	6.3 nM Compound: 13, A-1331852	Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay	[PMID: 33062160]
RS4-11	EC₅₀	> 5 μM Compound: 33; A-1331852	Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay	[PMID: 26988306]
RS4-11	EC₅₀	> 5000 nM Compound: 13, A-1331852	Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay	[PMID: 33062160]

In Vitro

A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells with IC₅₀s in the low nanomolar range but does not affect MEF cells lacking BAK or BAX. In CellTiter-Glo cell viability assay, A-1331852 inhibits NCI-H847, NCI-H1417, SET-2, HEL, OCI-M2 with EC₅₀ values of 3, 7, 80, 120 and 100 nM^[1].

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

In Vivo

A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent. Additionally, A-1331852 combines with venetoclax to recapitulate the efficacy of navitoclax in the NCI-H1963.FP5 xenograft model of SCLC. A-1331852 significantly inhibits tumor growth in seven subcutaneous xenograft models of solid tumors, including breast cancer, NSCLC, and ovarian cancer^[1].

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

Molecular Weight

658.81

Formula

C₃₈H₃₈N₆O₃S

CAS No.

1430844-80-6

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=NC(N2CC3=C(C=CC=C3C(NC4=NC5=CC=CC=C5S4)=O)CC2)=CC=C1C6=C(C)N(CC7(C8)CC9CC8CC(C9)C7)N=C6)O

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 : ≥ 50 mg/mL (75.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 4 mg/mL (6.07 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5179 mL	7.5894 mL	15.1789 mL
5 mM	0.3036 mL	1.5179 mL	3.0358 mL
10 mM	0.1518 mL	0.7589 mL	1.5179 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:

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

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: 2.5% DMSO 10% Ethanol 27.5% PEG300 60% Phosal 50 PG
Solubility: ≥ 2.5 mg/mL (3.79 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (3.16 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.16 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (262 KB) LCMS (105 KB) Elemental Analysis Report (119 KB)

Handling Instructions (2659 KB)

References

[1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40. [Content Brief]

Cell Assay ^[1]	SCLC and AML cell lines are incubated with increasing concentrations of navitoclax, venetoclax, or A-1155463 for 48 hours before assessing cell viability. Cell killing EC₅₀ values are calculated^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: The growth inhibition of established tumors in SCID-bg mice is studied. A-1331852 is administered orally daily for 14 days at 25 mg/kg and RP-56976 is administered intravenously at 7.5 mg/kg. The change of tumor volume is monitored daily^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med. 2015 Mar 18;7(279):279ra40. [Content Brief]

Complete Stock Solution Preparation Table

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

Ethanol / DMSO	1 mM	1.5179 mL	7.5894 mL	15.1789 mL	37.9472 mL
Ethanol / DMSO	5 mM	0.3036 mL	1.5179 mL	3.0358 mL	7.5894 mL
DMSO	10 mM	0.1518 mL	0.7589 mL	1.5179 mL	3.7947 mL
	15 mM	0.1012 mL	0.5060 mL	1.0119 mL	2.5298 mL
	20 mM	0.0759 mL	0.3795 mL	0.7589 mL	1.8974 mL
	25 mM	0.0607 mL	0.3036 mL	0.6072 mL	1.5179 mL
	30 mM	0.0506 mL	0.2530 mL	0.5060 mL	1.2649 mL
	40 mM	0.0379 mL	0.1897 mL	0.3795 mL	0.9487 mL
	50 mM	0.0304 mL	0.1518 mL	0.3036 mL	0.7589 mL
	60 mM	0.0253 mL	0.1265 mL	0.2530 mL	0.6325 mL

A-1331852 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-13318521430844-80-6A1331852A 1331852Bcl-2 FamilyInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

A-1331852

Customer Review

A-1331852 Related Antibodies

33 Publications Citing Use of MCE A-1331852

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bcl-2 Family Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

A-1331852 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

A-1331852 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report