A-1331852 纯度:99.21% 100mg

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首页酶、辅酶及抑制剂MCE>

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A-1331852 纯度:99.21% 100mg

市场价：: 14000.00

促销价：: ¥14000.00

货号：HY-19741

品牌：MCE

配送至：

北京朝阳

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支 (预计4-5工作日到货(以MCE官网货期为准))

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商品介绍
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A-1331852是具有口服活性的BCL-XL选择性抑制剂，K_i值小于10 pM。

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)

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].

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].

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (75.89 mM)

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (3.79 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (3.79 mM); Suspended solution
3.

Add each solvent one by one: 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.79 mM); Clear solution

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.

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 docetaxel 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.