CREB-IN-1 TFA | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CREB-IN-1 TFA

CREB-IN-1 TFA 是一种有效的，具有口服活性的 CREB 抑制剂 (IC₅₀=0.18 µM)。CREB-IN-1 TFA 能够抑制乳腺癌细胞的生长。

CREB-IN-1 TFA Chemical Structure

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC₅₀=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth^[1].

IC₅₀ & Target

IC₅₀: 0.18 µM (CREB)^[1]

体外研究
(In Vitro)

CREB-IN-1 TFA (compound 3) (HEK 293T cells; 100 µM; 24 hours) inhibits CREB-mediated gene transcription with an IC₅₀ of 0.18 µM^[1].
CREB-IN-1 TFA (100 µM; 3 days) shows potent activities in MDA-MB-231 (GI₅₀=0.38 µM) and MDA-MB-468 (GI₅₀=0.021 µM) cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	HEK 293T cells
Concentration:	100 µM
Incubation Time:	24 hours
Result:	Inhibited CREB-mediated gene transcription with an IC₅₀ of 0.18 µM.

Cell Proliferation Assay^[1]

Cell Line:	MDA-MB-231, MDA-MB-468 cells
Concentration:	100 µM
Incubation Time:	3 days
Result:	Showed potent activities in MDA-MB-231 (GI₅₀ =0.38 µM) and MDA-MB-468 (GI₅₀ =0.021 µM) cells.

体内研究
(In Vivo)

CREB-IN-1 TFA (5, 10, 20 mg/kg) shows much improve oral bioavailability at 38%^[1].
Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice ^[1].

route	dose(mg/kg)	t_1/2(h)	T_max(h)	C_max(ng/mL)	AUC_0-t(ng·hr/mL)	AUC_0-∞((ng·hr/mL)	bioavailability (F%)
IP	10	4.2	1.0	156	892	910	144
PO	20	5.5	2.00	73	468	479	38

Mice, 5 mg/kg IV; 10 mg/kg IP; 20 mg/kg PO^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female C57BL/6 mice^[1]
Dosage:	5, 10, 20 mg/kg (dissolved in 0.1 N NaOH in ddI H₂O at 40 mg/mL and further dilutions were made using ddI H₂O)
Administration:	Showed much improve oral bioavailability at 38%.
Result:	Showed much improve oral bioavailability at 38%.

分子量

778.06

Formula

C₃₅H₃₂ClF₃N₃O₁₀P

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Peng J, et al. Design, Synthesis and Biological Evaluation of Prodrugs of 666-15 as Inhibitors of CREB-Mediated Gene Transcription. ACS Med Chem Lett. 2022; 13(3):388-395.

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